Hydrolysis Rate Constants for Enhancing
   Property-Reactivity Relationships

                   by
          J.  Jackson  Ellington
          Measurements Branch
   Environmental Research Laboratory
         Athens, GA 30613-7799
   ENVIRONMENTAL RESEARCH LABORATORY
   OFFICE  OF  RESEARCH AND DEVELOPMENT
 U.S.  ENVIRONMENTAL PROTECTION AGENCY
         ATHENS, GA 30613-7799

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                            DISCLAIMER







     The information in this document has  been funded wtaily anr



in part by the United States Environmental Protection Ajeney.   It



has been subject to the Agency's peer and  administrative re-wifflw,,



and it has been approved for publication as an EPA document.



Mention of trade names or commercial products  does not const drttmtte



endorsement or recommendation for use by the U.S.  Environmental!



Protection Agency.
                                ii

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                             FOREWORD



     As environmental controls become more expensive and

penalties for judgement errors become more severe, environmental

management requires more precise assessment tools based on

greater knowledge of relevant phenomena.  As a part of this

Laboratory's research on occurrence, movement, transformation,

impact, and control of chemical contaminants, the Measurements

Branch determines the occurrence of unsuspected organic

pollutants in the aquatic environment and develops and applies

techniques to measure physical, chemical, and microbial

transformation and equilibrium constants for use in assessment

models and for development of property-reactivity correlations.

     In response to the land banning provision of the 1984

Hazardous and Solid Waste Amendments to PL 98-616, the Resource

Conservation and Recovery Act (RCRA),  a mathematical model was

developed to estimate potential groundwater contamination from

chemicals placed in land disposal sites.  Application of the

model requires as input the hydrolysis rate constant(s) for

chemical(s) of concern.  Measured hydrolysis rate constants and

the development of property-reactivity correlations to predict

them for similar chemicals are discussed relative to their

potential application to new chemicals being considered by EPA's

Office of Solid Waste for regulation.

                    Rosemarie C. Russo, Ph.D.
                    Director
                    Environmental Research Laboratory, Athens, GA
                               iii

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                            ABSTRACT







     This report examines the rate constants for hydrolysis in



water of 10 classes of organic compounds with the objective of



establishing new or expanding existing property-reactivity



correlations.  These relationships can then be used to predict



the environmental hydrolysis fate of chemicals that have similar



molecular structure.  The compound classes covered by this report



include:  aliphatic and aromatic carboxylate esters, alkyl and



aromatic halides, amides, carbamates,  epoxides, nitriles,



phosphate esters, alkylating agents, halogenated ethers, and



oxidized sulfur compounds.  Three predictive techniques (one



based on empirical correlations with derived constants, another



using infrared spectra and a third relying on fundamental



calculations requiring only chemical structure) were used to



predict and compare hydrolysis rate constants for simple alkyl



esters.  The predicted rate constants were generally within a



factor of two of each other and the laboratory-determined values.

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                             Contents

                                                            Page

Foreword                                                    iii

Abstract                                                     iv

List of Tables and Illustrations                             vi

Acknowledgments                                             vii



1.    Introduction                                             1

2.    Property-Reactivity Correlations (PRCs)                  2
       and Prediction Programs

3.    Hydrolysis Background                                    3


4.    Hydrolysis Rate Constants and Half-Lives                 7
       at pH 7 and 25°C

     4.1   Aliphatic and Aromatic Carboxylate Esters          7
     4.2   Alkyl and Aromatic Halides                        11
           A.  Chlorinated Alkyls                            11
           B.  Brominated Alkyls                             13
           C.  Bifunctional Chloroalkanes                    14
           D.  Polycyclic and Aromatic Halogenated
                 Hydrocarbons                                15
     4.3   Amides (Primary and N-Substituted)                20
     4.4   Carbamates                                        23
     4.5   Epoxides                                          26
     4.6   Nitriles                                          29
     4.7   Phosphate Esters                                  31
     4.8   Alkylating Agents                                 35
     4.9   Halogenated Ethers                                38
     4.10  Oxidized Sulfur Compounds                         40
     4.11  Other Miscellaneous Compounds                     43

5.    Predictive Techniques                                   46

6.    References                                              49

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                  List of Tables and  Illustrations


                                                            Page
Tables
 1.  Aliphatic and Aromatic Carboxylate Esters                9
 2.  Alkyl and Aromatic Halides                           16,17,18
 3.  Primary and N-Substituted Amides                        21
 4.  Carbamates                                              24
 5.  Epoxides                                                27
 6.  Nitriles                                                30
 7.  Phosphate Esters                                        33
 8.  Alkylating Agents                                       36
 9.  Halogenated Ethers                                      39
10.  Oxidized Sulfur Compounds                               41
11.  Miscellaneous Compounds                               44,45
12.  Predicted and Laboratory-Determined Hydrolysis Rate
       Constants of Carboxylate Esters                       47


Illustrations

 1.  Aliphatic and Aromatic Carboxylate Esters               10
 2.  Alkyl and Aromatic Halides                              19
 3.  Primary and N-Substituted Amides                        22
 4.  Carbamates                                              25
 5.  Epoxides                                                28
 6.  Phosphate Esters                                        34
 7.  Alkylating Agents                                       37
 8.  Oxidized Sulfur Compounds                               42
 9.  SPARC Generated pH-rate Profile of Methyl Methacrylate  48
                               VI

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                         Acknowledgments







     The assistance of Ms. Cheryl Trusty in preparation of the



draft manuscript, figures, and tables is gratefully acknowledged.



Ms Mimi Houston's effort in retyping the draft and subsequent



revisions was always timely and professional.  The review of the



manuscript by Drs. Peter Jeffers and Timothy Collete is also



gratefully acknowledged.
                               VII

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             Hydrolysis Rate Constants for Enhancing



                Property Reactivity Relationships
1.0  Introduction



     Each year more than 1000 new chemicals are introduced into



commerce and thus into the environment worldwide.   Regulators and



scientists need reliable data on the persistence,  mobility,



toxicity and possible risk to humans or the ecosystem associated



with these new chemicals as well as the more than 65,000



currently in use (1).  The possible persistence of these



chemicals and accompanying risk of exposure to humans and other



species of concern has resulted in a demand on regulators to



provide effective techniques for quantifying their mobility and



fate.



     As part of the effort to evaluate potential mobility and



fate associated with chemical constituents of wastes under



consideration for land disposal, EPA's Office of Solid Waste



(OSW) uses a relatively simple model to estimate potential



groundwater contamination at specified withdrawal points in



proximity to a landfill.  This model calculates horizontal



chemical movement in the aquifer based on advection, dispersion,



sorption and transformation.  Hydrolysis is the only



transformation process specifically considered at this time.



     To apply this model to chemicals of interest to OSW,



hydrolysis rate constants for 98 chemicals were previously



obtained either from literature sources or laboratory

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determinations (2-4) using protocols developed at ERL-Athens  (5).
     The objective of this report was to examine the rate data
presented in references 2-4 and organize them by compound class,
with the goal of either enhancing existing property-reactivity
correlations (PRCs) or developing new PRCs if sufficient data
have been generated for a particular class of chemicals.  These
correlations then can be applied to new chemicals in wastes being
considered by OSW for regulation.
2.0  Property Reactivity Correlations (PRCs) and Prediction
Programs
     The use of PRCs for predicting rate and equilibrium
constants for organic reactions is well established (6).
Pharmaceutical and pesticide manufacturers routinely use
historical data on existing compounds in designing new products
to either increase or decrease potency and/or persistence while
decreasing or eliminating unwanted side effects.  Any chemical
released to the environment is subjected to a wide variety of
conditions that can transform it to a different product.  PRCs
offer a means for estimating kinetic constants for important
transformation processes such as hydrolysis, photolysis, and
redox reactions.
     For example, a symposium, "Structure-Activity Relationships
in Environmental Toxicology and Chemistry" was part of the
American Chemical Society Meeting April 6-8,1987, in Denver,
Colorado.    The symposium topics included SARs to estimate rate
constants for oxidation by HO* radicals  in the troposphere and
peroxy radical and singlet oxygen reactions in surface waters,

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and to estimate salinity constants for ligands and selected metal
ions.  Several SARs correlated molecular structure with toxicity
to aquatic organisms.
     The reliability of any PRC/SAR is directly related to the
accuracy of data input and to how well the selected data
represent the particular process.  Most existing PRCs are
empirical correlations (based on derived measures of the polar
and/or steric effects of compound structure) that predict new
kinetic constants only for reaction pathways for which data exist
for similar transformations.  Using this approach, Drossman,
Johnson and Mill developed SARs for base-promoted hydrolysis of
esters and carbamates using a*  and Es values for the compounds of
interest (7).
     Two approaches that are less dependent on measured kinetic
data are being developed at ERL-Athens.  Collette (8) is
developing a method for predicting environmental fate constants
of chemicals based on their infrared spectra.   Even though many
reactivity parameters may be amenable to this approach, to date,
only alkaline hydrolysis of organic esters has been considered in
depth.  Karickhoff et al. (9) is developing a prototype computer
program SPARC (SPARC Performs Automated Reasoning in Chemistry)
that uses computational alogrithms based on fundamental chemical
structure theory.  This allows estimation of values for a broad
variety of reactivity parameters both kinetic and equilibrium: Uv
light absorption, pKa, and various reaction rate constants, or
any parameters that depend on molecular structure.  The agreement
of the alkaline hydrolysis rate constants for carboxylate esters

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calculated by all of the  above  methods as well as determinedE im

the laboratory will be discussed  in more detail later.

3.0  Hydrolysis Background

     Hydrolysis of organic compounds refers to reaction of t2us>

compound with water in which bonds  are broken and new bonds

HO- and H- are formed.  A common  example is the react ion of ant

alkyl halide with water resulting in the loss of halide lore (,-



          RX + HOH - > ROH + HX  (or H*,  X')



     The rate of the reaction may be promoted by the hydrondum

ion (H+,  or H3O+)  or the hydroxyl  ion (OH") .  The former is

referred to as specific acid catalysis and the latter as
base catalysis.  These two processes  together with the neviititaJ!

water reaction were the only mechanisms  considered in lefesrenxD

2-5.



     Some chemicals show a pH-dependent  elimination reactions

          H   X
          II    H+ or
        - C - C -  - >  C = C + HX
                    OH"

For the hydrolysis rate constants  reported in references  2>-5>t

only the disappearance of substrate was  monitored with no

attempts to identify mechanisms.

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     If all processes referred  to  as  hydrolysis are included, the

rate of hydrolysis is given by  the equation,

    d[C]
     dt
         = kjc]  =  kA[H*][C]  +
where [C] is the concentration of reactant and k,, is the  observed

pseudo-first-order rate constant at  a  specific pH and

temperature, kA, kg,  and k,,1 are second-order rate constants for

the acid, base  and neutral promoted  processes,  respectively.  The

water concentration  is essentially not depleted by  the reaction

and is much greater  than  [C], thus k^tHjO] is  a constant (k^,) ,

the pseudo-first order neutral rate  constant.

     Equation 1 assumes each individual rate process  is first

order in substrate,  thus  k,, can be defined as:




     kj,  = kA[H+] + kgCOlf]  + k,                                (2)
     Equation 1 then becomes simply,

        d[C]
                                                             (3)
         dt
     which integrates to

     [C]t = [C]0 exp^t)                                    (4)
     or
        [C]t
     In - = k,,t                                           (5)
        [C]0

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     Equation 5 allows calculation of the concentration of a

reactant at any time (t).   Specifically, when [C]t = h[C]0,

equation 5 reduces to:


              lnT
                 50    In 2   0.693
     t = t.h = 	 = 	 = 	                          (6)
     For many chemicals, hydrolysis can be the dominant pathway

for degradation in the environment.  Functional groups that are

potentially susceptible to hydrolysis are:

           1.  Aliphatic and aromatic carboxylate esters
           2.  Alkyl and aromatic halides
           3.  Amides
           4.  Carbamates
           5.  Epoxides
           6.  Nitriles
           7.  Phosphate esters
           8.  Alkylating agents
           9.  Halogenated ethers
          10.  Oxidized sulfur compounds

     Tables 1 through 10 contain hydrolysis rate constant data

and half-lives for chemicals in the above classes at pH 7 in

aqueous solution at 25°C.   The corresponding figures contain

structures of selected chemicals in these classes.  The data in

Tables 1 through 10 were either reported in references 2-4 or

extracted from the indicated references for comparison purposes.

For data generated at other temperatures, the rate constants were

extrapolated to 25°C using either the experimentally-determined

activation energies for each chemical, or an assumed activation

energy (Ea)  of 20  kcal/mol for each path (acid,  neutral,  or base

hydrolysis).  Since the majority of compounds have measured Ea

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values in the range of 15 to 25 kcal/mol, the assumption of 20



kcal/mol for Ea generally introduce  less  than an order of



magnitude error in the extrapolated rate constant.



     Mabey and Mill (10)  completed a critical review of the



hydrolysis of organic compounds in water under environmental



conditions.  Hydrolysis rate constant values from Mabey and Mill



are herein used, where available, for comparison purposes.



4.0  Hydrolysis Rate Constants and Half-Lives at pH 7 and 25"C



4.1  Aliphatic and Aromatic Carboxylate Esters



     Table 1 summarizes data for hydrolysis of aliphatic and



aromatic esters at 25°C and pH 7.  For these compounds,  hydrolysis



at pH 7 is dominated by hydroxide ion for simple alkyl and



aromatic esters (10).  Thus, the values of kg yield a reliable



calculation of k,,  and half-lives at  pH 7.   For more structurally



complex esters and esters with substitutents that reduce the



electron density of the carbonyl carbon (a-halogenated) neutral



hydrolysis (k,,)  will be competitive  at pH 7.   The general rule is



that methyl esters are twice as reactive as other n-alkyl esters



and branching on the a-carbon on either side of the carboxylate



group will retard hydrolysis by factors of three to ten  (7).



     The above effects (i.e., the reduction of electron density by



the phenyl substituent and methyl versus ethyl ester) are evident



in the factor of eight increase in 2,4-D methyl ester hydrolysis



rate compared to ethyl methoxyacetate.  The 2,4-D methyl ester was



used as a standard reference compound and the reported rate



constant is the mean of 27 determinations.  Lasiocarpine and



reserpine are structurally complex molecules that have two

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hydrolyzable groups (labeled 1 and 2 in Figure 1).  Site 1 in



lasiocarpine is structurally similar to methyl methacrylate and



site 2 is structurally similar to ethyl glycolate.  Branching on



the o-carbon at site 2 (potentially the most easily hydrolyzed)



retards hydrolysis to the extent that disappearance is dominated



by neutral hydrolysis.  Similarly, in reserpine,  branching on the



acyl carbon at site 1 (compare with methyl acetate) retards



hydrolysis by hydroxide ion to the extent that neutral hydrolysis



is again dominant at pH 7.  Addition of a methyl group to the a-



carbon of the acyl group of methyl acrylate (11)  to form methyl



methacrylate decreases the kg  by a factor of two.   The small  kg



for di-n-octylphthalate is consistent with increasing chain length



in the alcohol group (8).
                                8

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                              TABLE 1. ALIPHATIC AND ARCMATIC GAEBOXXIATE ESTERS
                                                  Rate Constants (25'C)
CAS Number
Compound
 -
M -  hr
Neutral
 hr"1
M   hr
Calculated  Ref.
Half-Life
pH 7, 25°C
1928-38-7   2,4-D Methyl ester

3938-96-3   Ethyl nethoxyacetate

            Ethyl glyoolate

303-34-4    lasiocarpine

96-33-3     Methyl acrylate

79-20-9     Methyl acetate

50-55-5     Reserpine

93-89-0     Ethyl benzoate

80-62-6     Methyl roethacrylate

84-66-2     Diethylphthalate

84-74-2     Ditoutylphthalate

117-84-0    Di-n-Octylphthalate
                                                  41,000 ± 5,000     7d       4

                                                      4968          58d       7

                                                      3636          79d       7

                                    (4.9 ± 0.1JE-5   9.8 ± 0.1      1.6y      3

                                                      406a          1.9y     11

                                                      655           1.2y      7

                                    (4.5 ± 1.8)E-5  9.8 ± 11        1.7y      2

                                                      105           7.5y      7

                                                   200 ± 47         3.9y      3

                                                      90            8.8y      8

                                                      36             22y      8

                                                      7.4           107y      3
a.  Assumed E& = 20 kcal/mol in extrapolating kg fron 30°C to 25°C.

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                                         o
                                              O-CH3
                        2,4-D Methyl ester
                                        Oft,
                                   HC
OH
                                                   CH3
                                        OH  o-CH,
                        Lasiocarpine
H3CO
                                                              OCH*
                                                               OCH,
                      ;   o
            Figure 1. Aliphatic and Aromatic Carboxylate Esters
                                    10

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4.2  Alkyl and Aromatic Halides
     The halogenated compounds in Table 2 range in complexity from
the simple chloroethane to the multihalogenated polycyclics such
as aldrin.  All have in common the potential hydroxide ion or
water mediated cleavage of the carbon-halogen bond to give
alcohols.  E2 elimination to give olefins and hydrogen halides,
although not true hydrolysis, can occur in water and may be
enhanced by increasing hydroxide ion concentration and
temperature.  Elimination is treated as hydrolysis in the present
text.  Multifunctional halogenated chemicals (such as halogenated
ethers and nitriles) are also included in Table 2 because the
point of attack for these compounds is also the carbon-halogen
bond.  Table 2 is subdivided into the four groups: chlorinated
alkyls, brominated alkyls, bifunctional chloroalkanes, and
polycyclic and aromatic hydrocarbons.
     A.  Chlorinated Alkyls (Table 2. Figure 2)
     Allyl halides such as allyl chloride are known to hydrolyze
rapidly by a neutral mechanism.  Both chlorines in cis and trans-
l/4-dichloro-2-butene (DCB) are allylic.  Therefore, because this
compound has two equally reactive groups per molecule, the
disappearance rate constant for the DCBs should be larger than
that for allyl chloride.  It is, in fact, larger by a factor of
20.  Pentachlorocyclohexene (PCCH) has a chlorine on the gamma
carbon of the allyl fragment.  The gamma chlorine on PCCH retards
formation of the carbonium ion and subsequent reaction of the
allylic chlorine by an order of magnitude (half-life =2.1 years).
 Benzyl chloride was used as a standard reference compound in the
laboratory determination of hydrolysis rate constants for selected
                               11

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justified but probably preferred to the uniform assumption of a 20
kcal/mole activation energy.
     A second gem-dihalide  (p,p'-DDD)  undergoes slow neutral
hydrolysis (half-life 28 years), apparently due to
steric/electronic interferences from the two ^-chlorinated phenyls
on the a-carbon (Figure 2).   Jeffers reported that a gem-dihalide
with a H-atom on the gem-substituted carbon (1,1-DCA) undergoes
slow neutral hydrolysis in comparison with the perhalogenated gem-
dichloride (2,2-DCP).   The methyl group in 1,2-dichloropropane
(1,2 DCP) increases the reactivity by a factor of five versus 1,2-
dichloroethane (1,2 DCA).  The third chlorine in 1,2,3-
trichloropropane decreases the hydrolysis rate by a factor of
three versus versus that of 1,2 DCP.  The fully chlorinated
hexachloroethane is almost totally resistant to hydrolysis.
     B.  Brominated Alkyls
     The reactivity of the vicinal bromines in the three
brominated alkyls studied should determine the hydrolysis
disappearance rate constants.  The factor of nine greater
reactivity of ethylene dibromide (EDB) over 1,2-dichloroethane
(Table 2 Section a) illustrates the increased susceptibility of
brominated compounds to hydrolysis.  Statistically, tris(2,3-
dibromopropyl)phosphate (Tris) with three vicinal bromine centers
should have a larger k,, than ethylene  dibromide.   The two k,,
values are almost identical, however,  which leaves alkaline
hydrolysis (kg)  of the phosphate ester as the  determining factor
for the shorter half-life (4.4y) compared to EDB  (8y).
Apparently, disappearance of l,2-dibromo-3-chloropropane  (DBCP) is
controlled by hydroxide-ion-mediated dehydrobromination  (E2
                                12

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Appendix VIII chemicals (5).  The standard rate constant value in



Table 2 is the average of 28 determinations and agrees well with



the value of 4.6 E-2 h"1 in Mabey and Mill  (10).  Hydrolysis of



benzyl chloride is similar to that of the allyl chlorides in that



the rate is enhanced by the ease of formation of a reactive



carbonium ion.



     Jeffers (12) and Queen and Robertson (13) independently



determined that gem-dihalides are unreactive to nucleophilic



displacement by hydroxide ion but both measured a neutral



hydrolysis rate constant (attack by water) and activation energy



for 2,2-dichloropropane.  Jeffers1 and Queen and Robertson's kN



values are approximately a factor of 2 lower than our value (4) .



Our rate was determined at 45°C,  however,  and extrapolated to  25°C



using an assumed activation energy of 20 kcal/mol.  If Jeffers'



average value of 25.2 kcal/mol for neutral hydrolysis of



chlorinated alkyls is used to extrapolate our rate from 45°C,  we



obtain a value of 2.4±0.12 E-2h~1, which is within experimental



error of Queen and Robertson's (13) value of 2.44 E-2 h"1  (who



reported an activation energy of 26.6 kcal/mol).



     Jeffers (12) reported the hydrolysis rate constants for 18



chlorinated methanes, ethanes, ethenes, and propanes that were



measured in dilute aqueous solutions within the temperature range



of 0 to 180°C and at pH values from 3  to 14.   The average of



neutral activation energies reported by Jeffers was 25.2±2.87



kcal/mol whereas the average for 15 basic activation energies was



26.2±3.87 kcal/mol.  Thus, for chlorinated alkanes when the



activation energy is unknown, use of Jeffers1 values to



extrapolate rates to other temperatures would not only be
                               13

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elimination) as evidenced by the kg term,  whereas for another



similarly substituted trihaloalkyl, 1,2,3 trichloropropane (Table



2, Section a), disappearance is dominated by reaction with water



(k,,) .   The electronegative chlorine on the



/3-carbon in DBCP apparently enhances elimination of HBr to make



dehydrobromination the dominant pathway at pH 7.



     C.  Bifunctional Chloroalkanes



     The halogenated alkanes in this group contain either



hydroxyl, cyano, or the ether linkage as the second functional



group.  The two chloropropanols (1,3-DCA and 2,3-DCA) differ in



reactivity by two orders of magnitude.  As a first approximation,



one might expect that the reactivity of 1,3-DCA should be



comparable to 1,3-dichloropropane  (1,3-DCP), but the observed rate



constant for 1,3-DCP is closer to the value of 2,3-DCA.  The



enhanced reactivity of 1,3-DCA can be attributed to the 2-hydroxyl



group.  Electronegative substituents on the /3-carbon are known to



enhance reactivity of a-halogens (13).  Additionally, the acid



character of the hydroxyl is enhanced by the two chlorines.  The



oxyanion resulting from ionization of the weak acid can, through



intramolecular cyclization, displace either adjacent chlorine to



form epichlorohydrin, a reactive intermediate.  Similar ionization



and cyclization enhances the reactivity of 2-chloroethanol (2-CE)



versus 1,2-dichloroethane  (1,2-DCA).  The 2,3-DCA contains vicinal



chlorines but the hydroxyl substituent enhances reactivity by only



one order of magnitude over 1,2-DCA.



     The bis-dichloroethyl ether (DCE) reactivity, as expected,



was similar to that of ethyl chloride.  The 2-(2-chloroethoxy)



ethanol  (CEE) with one less reactive chlorine than DCE has a
                                14

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slightly enhanced rate over DCE, again due to intramolecular



oxyanion displacement of the chlorine to form the cyclic dioxane.



The oxygen substituent on the a-carbon of chloromethyl methyl



ether enhances reactivity by six orders of magnitude over bis-



dichloroethyl ether.  The ease of formation and stability of the



methoxymethyl carbonium ion has been proposed to explain the



enhanced reactivity of chloromethyl ethers (20) over chlorethyl



ethers.



     D.   Polycylic and Aromatic Halogenated Hydrocarbons



     The halogenated polycyclic and aromatic hydrocarbons comprise



a very persistent group of chemicals in the environment.  The



three most reactive polycyclic compounds studied (Aldrin,



Dieldrin, and Isodrin) all contain a perchlorinated gem-dichloro



carbon.   Dieldrin (Aldrin epoxide) also contains an epoxide



oxygen,  and, with two reactive centers, would be expected to have



the shortest half-life.  Apparently hydrolysis of the epoxide is



stericly hindered and the orientation of the cyclic ring is such



that hydrolysis of the gem-dihalide also is retarded in comparison



to 1,2-DCP.



     Structural orientation is also the reason that the cis isomer



of chlordane is more susceptible to hydroxide-ion-mediated



dehydrohalogenation.  The 1-exo, 2-exo orientation of the chlorine



atoms in cis-chlordane facilitates the E2 elimination of HC1.  No



disappearance of trans-chlordane was observed under the same



conditions.  All the chlorinated aromatics studied were very



stable to hydrolysis.
                                  15

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TABLE 2. AIK¥L AND ARCMAXIC
CAS Number

Ccnpound M hr
Rate Constants (25'C)
Neutral Base
hr'1 M"1 hr'1
Calculated
Half-life
pH 7, 25°C
Ref.
a. CHLORINATED ALKYIS
107-05-1
764-41-0
110-57-6
319-94-8
100-44-7
594-20-7


72-54-8

58-89-9
78-87-5
107-06-2
96-18-4
67-72-1
Allyl Chloride
cis-1 , 4-Dichloro-2-butene
trans-1 , 4-Dichloro-2-butene
Pentachlorocychlohexene (PCCH)
Benzyl Chloride
2,2-Dichloropropane (2,2-DCP)


p,p'DDD
1,1-Dichloroethane (1,1-DCA)
Lindane
1 , 2-Dichloropropane
1,2-Dichlorethane (1,2-DCA)
1,2, 3-Trichloropropane
Hexachloroethane
4.6E-4
(9.1 ± l.l)E-3
(9.0 ± 0.5JE-3
3.0E-5 74 ± 3
(5.1 ± 0.3JE-2
(4.7 ± 0.2)E-2
1.9E-2
2.4E-2
(2.8 ± 0.9)E-6 5.2
1.29E-6 4.32E-5
(1.2 ± 0.2)E-4 198 ± 6
(5.0 ± 0.2)E-6 4.3E-4
1.1E-6
(1.8 ± 0.6)E-6 9.9E-4
4.3E-7
63d
3.2d
3.2d
2.1y
14h
15h
36h
29h
28y
61y
207d
15. 8y
72y
44y
1.8E9
10
2
2
4
4
4
12
13
3
12
3
3
12
2
12

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                                    T&HCE 2. MK£L AND ARCMATIC HAUDES - continued
CAS Number
b. BRCMINA
106-93-4
126-72-7
92-12-8

Ccopcund M hr
TTD AUKANES
Ethylene dibrcmidfp (FOB)


,2-DiDrcBO— 3-cxiJLorppropane (DBCP;
Rate Constants (25°a
Neutral Base
nr"1 M"1 hr"1
9.9E-6
tris) (1.0 ± 1.1) E-5 78
20.6
Calculated Bef.
Half-life
pH 7, 25'C
8y 14
4.4y 3
38y 2
C.  ETFUNCTIONAL CHDORQAIJ^ANES



142-28-9    1,3-Dichlcjroprupane (1,3-DCP)



96-23-1     l,3-Dichlaro-2^jrcpanol (1,3-DCA)



616-23-9    2,3^idiLoro-l-^rapanol (2,3-DCA)



542-76-7    3-ChlorDpropanenitrile



Hl-44-4    bis-Dichloroethylether (DCE)



628-89-7    2-(2-Qaaroethoxy)ethanol (GEE)



107-07-3    2-Chloroethanol (2-CE)



75-00-3     Ethyl chloride



107-30-2    Chloranethyl methylether
   3.5E-5          1E-3         2.3y       12




(3.1 ± 0.2)E-3    850 ±  87      9.Id       2




(5.3 ± 0.8JE-5    20.6 ± 2.2    1.4y       2




(1.3 ± 0.1JE-4  12,071 ± 1,960  22d       3




(2.6 ± 0.1JE-5                 3.0y       3




(3.2 ± 0.1)E-5                 2.5y       4




   4.5E-6            36       9.8y       4




   4.5E-5                      1.8y      15




    21                       2 min      20

-------
CO
M/AEM^*; ^ » AJLJ^IVlLf ANo /VRCMAJ.JLO HAJLJLOEjS continued.
CAS Number
Pate Constants (25°C>
Acid Neutral Base
Compound M"1 hr'1 hr"1 M'1 hr"1
Calculated
Half-Life
pH 7, 25°C
Ref.
d. POLSfCYCLTC AND ARCMftTIC HAIOGENMED HYDROCARBONS
60-57-1
28291-10-3
309-00-2
465-73-6
5103-74-2
5103-71-9
108-90-7
95-50-1
541-73-1
106-46-7
24009-05-0
608-93-5
95-94-3
88-06-2
101-14-4
Dieldrin (7.5 ± 3.3)E-6
DL-trans-4-ChlorostiIbene
Oxide 1080 ± 108 (61 ± 7.2)E-4
Aldrin (3.8 ± 2.3)E-5
Isodrin 1.7E-6
Cis-chlordane 4.3E-3
trans-Chlordane zero hydrolysis after 5 days at 85 °C, pH
Chlorobenzenea <0 . 9
1, 2-Dichlorobenzenea <0 . 9
1 , 3-Dichlorobenzenea <0 . 9
l,4-Didtilorobenzenea <0.9
lHHydroxychlordeneb <1 x 10-4
Pentadilorobenzenea <0.9
l,2,4,5-Tetrachlorobenzenea <0.9
2,4,6-Trichlorophenolc (2.3 ± 3.5)E-7
4 , 4-^fethvlene-bis- (2-Chloroaniline) <9E-8
10. 5y
112h
760d
46y
>184,000
11
>900y
>900y
>900y
>900y
200,000y
>900y
>900y
>300y
>800y
2
4, 16
2
3
3

4
4
4
4
4
4
4
4
2
              a.    Based on assumed base mediated 1% disappearance after 16d at 85eC and pH 9.70  (pH 11.26 at room
                    temperature).
              b.    Based on assumed base mediated 5% disappearance after 48d at 85°C and pH 9.71  (pH 11.04 at room
                    temperature).
              c.    Based on assumed 5% disappearance after 330 hr at 85 °C.

-------
                                                                                        Cl
                              Pentachlorocyclohexene (PCCH)
                                                                        Lindane
       (Br-CH2-CHBr-CH2-O)3-P = O
      Tris(2,3-dibromopropyl)phosphate
                      N
                                                                H
                                                                      H
                                                                            Cl
                               H
                                                                      H
                                                       3-Chloropropanenitrile
Cl     Cl
         Dieldrin
Cl
                                   \
        Cl
          Aldrin
Isodrin
                        Cl
                           H
             Cl
               cis-Chlordane
                                   HC1
                          trans-Chlordane
                             Figure!. Alkyl and Aromatic Halides
                                            19

-------
4.3  Amides (Primary and N-Substituted)
     Amides generally hydrolyze by acid- nnd baso-m«d Lit i>d
processes to carboxylla no Ids and amines.  When the ratos
determined at pH's 3 and 7 or pH's 11 and 7 were the snmo, the
rate was reported as the neutral rate constant.
     Table 3 summarlzoa the rite datti at pH 7 nnd 25°C foe nevoral
primary and N-substituted amides.  Thioacetamide  Illustrates tho
instability introduced when sulfur ia substituted for oxygon.
(Acetamide is the oxygen analog.)  Electronegative substltuents
(fluoro- and ohloroaoetamide) or subutitutientu that doloc.ilizo
the carbonyl electrons  (acrylamido) enhance reactivity of tho
amide.  Pronamide hydrolysis nlso is enhanced by tho
delocalization of electrons into the dichlorophony1 substituont.
                                20

-------
TABLE 3. FKEMARY AND N-SUBSTTUJTED AMIDES
CAS Number
a. PRIMARY
62-55-5
60-35-5
640-19-7
79-07-2
79-06-1
Rate
-!°id-i
Conpcund M hr

Thioacetamide (6.0 ± 0.06)E-2
Acetamide 3 . OE-2
2-Fluoroacetamide
2-Chloroacetamide 4 . OE-2
Acrylamide <3 . 6E-3 <
Constants (25°C)
Neutral
hr"1

(8.6 ± l.l)E-5

(3.3 ± 0.3)E-5

(2.1 ± 2.1)E-6
Calculated
Base Half-£ife
M'1 hr"1 pH 7, 258C

1.4 ± 0.09 336d
0.17 3,440y
2.4y
540 1.5y
>38y
Ref.

3
10
3
10
2
b. N-SUBSTTTOIED
23950-58-5
591-08-2
53-96-3
Pronamide 4.3E-3
N- (aminothioxonethyl) acetaitd.de
2-Acetylaminofluorene
<1.5E-5
(1.7 ± 0.2)E-5
2.3E-6
7.4E-2 >5y
1.5 ± 0.09 4.6y
6E-3 34y
2
3
3

-------
              NH2
 Thioacetamide
                                                  H
                                                          O
           H
           Acrylamide
             O
             NH2

2-Fluoroacetamide
                                                       H
                   CH
N-(Aminothioxomethyl)-Acetamide
                                  O
                               I
                               H
                        Pronaraide
                                             Cl
                                             Cl
                                             CH,
                   2-Acetylaminofluorene
           Figure 3. Primary and N-Substituted Amides
                                  22

-------
4.4  Carbamates



     Hydrolysis of carbamates proceeds by acidic, basic, or



neutral processes to give alcohols, amines, and carbon dioxide.



Half-lives of carbamates as illustrated in Table 4 vary from



seconds to centuries (10).  Mitomycin C contains among its



functional groups a carbamate, an aziridine, and a labile methoxy



group.  The rate limiting step in disappearance of mitomycin C is



expulsion of the methoxide prior to opening of the aziridine ring



(22, 23).  The half-life of mitomycin C is comparable to 2-



methylaziridine in Table 11.  Ethyl carbamate, contrary to most



carbamates, is not N-substituted.  The reactivity of ethyl



carbamate is comparable to the simple alkyl amides.
                                 23

-------
                                                              TABLE 4.  CARBAMAIES
Rate Constants (25° a Calculated Ref .
CAS Number Compound
Acid Neutral
M hr hr
Base Half-Life
M'1 hr"1 pH 7, 25°C
              50-07-7     Mitcmycin C



              51-79-6     Ethyl Carbamate



              2303-16-4   Diallate
4320
    1.8E-3           43




   <2.6E-7         1.1E-1




(1.2 ± 0.7JE-5    0.9 ± 0.4
12.9d   22, 23



>300y       2



 6.6y       3
to

-------
H,C
           Ethyl carbamate
          trans-Diallate
      Figure 4. Carbamates
              25

-------
4.5  Epoxides



     Hydrolysis of epoxides in acid, neutral or base catalyzed



reactions yields diols as the final product.  Epoxides are



reactive compounds with half-lives generally minutes to less than



15 days (10), see Table 5.  Aromatic or conjugated epoxides tend



to be more reactive than strictly aliphatic epoxides.  Acid-



catalyzed hydrolysis is sensitive to the stability of the



transient carbonium ion formed by protonation of the oxirane ring



and subsequent breaking of one of the carbon-oxygen bonds.  This



enhanced reactivity is reflected in the hydrolysis rate constant



of D.L-trans-4-chlorostilbene oxide (CSO).  The stability of



Dieldrin is possibly due to shielding of the oxirane group from



attack by water and to lower reactivity of alkyl epoxides.
                                   26

-------
                                                TABLE 5. EPOXEDES
                                        	Rate Constants  (25"C)	   Calculated  Ref.
                                          Acid           Neutral          Base     Half-Life
CAS Number        Oonpound              M"1 hr""1          hr"1          M"1 hr'1   pH 7, 25*C


28291-10-3  DEr-trans-4-Chlorostilbene
            Oxide                     1080 ± 108      (61 ± 7.2)E-4a                   112h   4, 16

60-57-1     Dieldrin                                  (7.5 ± 3.3)E-6                  10.5y      2


a.  Neutral rate from Reference 16.

-------
trans-4-chlorostilbene oxide
      Cl      Cl
                Dieldrin
          FigureS. Epoxides
                      28

-------
4.6  Nitriles



     The hydrolysis of nitriles normally takes place only in the



presence of either strong acids or strong bases.  In both cases,



amides are the first reaction products, but amides cannot be



isolated as intermediates unless their rate of hydrolysis is lower



than that of the parent nitrile.  Nitrile data, summarized in



Table 6, confirms the stability of the monofunctional alkyl



nitriles (acrylonitrile and acetonitrile) under environmental



conditions.  Malonitrile (1,1-dicyanomethane), by comparison, is



very labile to degradation even under neutral conditions.  This



can be attributed to the activation  (ionization) of the a-



hydrogens.  The anion formed is unstable and some form of cleavage



or hydrolysis occurs when malonitrile loses a proton to form the



monoanion.
                                   29

-------
                                                               TABLE 6.  NITRITES
              CAS Number
Ocropound
                                                                 Rate Constants (25'C)
 -
M   hr
Neutral
 hr"1
                                                                 Calculated  Ref.
                                                                 Half-life
 -S336-!
M *- hr *•   pH 7, 25°C
              109-77-3    Malorxanitrile
              75-05-8     Acetonitrile
              107-13-1    Acrylonitrile
                   (4.2 ± 0.3)E-2
               (1.30 ± 0.40)E-3   806 ± 45       21d      3
                                  5.8E-3    >130,000y    3
                              (6.1 ± 6.5)E-1  1220y      2
u>
o

-------
4.7  Phosphate Esters



     Organothiophosphate and organodithiophosphate triesters,



depending on the substituents, may undergo hydronium-ion-catalyzed



hydrolysis, hydroxide-ion-catalyzed hydrolysis and neutral



hydrolysis and are quite reactive species.  Under environmental



conditions, only the neutral and hydroxide-ion-mediated hydrolyses



are relevant as illustrated in Table 7.  Most phosphate pesticides



have the general structure:
where R = an alkyl group  (usually methyl or ethyl) and X = an



organic radical.  Hydrolysis involves cleavage of either the P-OX



(-SX) bond  (hydroxide ion and neutral) or the 0-X (S-X) bond



(hydronium  ion) depending on conditions.



     When sulfur is substituted for oxygen in the P=O position,



the rate of hydrolysis is decreased, whereas substitution of S for



O in the P-O-X position increases the rate of hydrolysis.  The



greater electronegativity of the oxygen atom in the P=0(S)



position enhances the positive character of the phosphorus atom



and thus the attraction for the electrons on the hydroxide ion or



the water molecule (17).



     In breaking the P-O(S) single bond, the mercaptide anion is a



better leaving group than the alkoxide.  Rates of hydrolysis are



therefore accelerated when S is substituted for O in this
                                 31

-------
position.  The second-order alkaline hydrolysis rate constants of



thioesters have been correlated to the pKa of the conjugate acid



of the leaving group by the relationship:



                    log k = m'pKa + c



where m is the slope and c the intercept (18).



     Using the m and c values from Wolfe (18), and conjugate acid



pKa values calculated (9) by SPARC  (2-hydroxypyrazine) or Perrin



[(19) p-N,N-dimethylsulfamoyl phenol], we calculated second-order



alkaline hydrolysis rate constants for O,O-diethyl-O-pyrazinyl



phosphorothioate and Famphur.  The calculated values in Table 7



agree within a factor of two with the laboratory-determined



values.  The hydrolysis of the trialkylthioester is an order of



magnitude slower than the above thioesters with at least one



aromatic substituent.



     The greater reactivity when 0 is replaced by S in the leaving



group is evidenced by the 50% increase in the neutral hydrolysis



rate constant of O,O,S-triethyl ester over the O,0,O-triethyl



ester.  The reactivity of the dithioesters Phorate and Dimethoate



is further enhanced by reactive groups in the alkyl side chain to



yield half-lives of less than five days  compared to a half-life of



115 days for Famphur.
                                 32

-------
                                                             TABIE 7. EHOSEHATE ESTERS
u>
CAS Number Compound
a. THIOESTERS
297-97-2 OfO-Diethyl-o-pyranzinyl
phosphorothioate
52-85-7 Fatnphur
126-68-1 O,O,O-Triethylester
phosphorothioic acid
b. DITHIOESTERS
298-02-2 Riorate
60-51-5 Diaethoate
298-04-4 Disulfoton
Rate Constants (25°a
Acid Neutral Base
M"1 hr"1 hr""1 M"1 hr"1

(1.0 ± 0.1JE-3 7.3 ± 0.7
3.8a
(2.5 ± 0.9)E-4 5.0
8.6a
(2.0 ± 0.2)E-5

7.2E-3
1.7E-4 756
(2.8 ± 0.4)E-4 5.99
Calculated Ref.
Half-life
pH 7, 258C

29d 3
calculated
115d 2
3.9y 3

96h 3
118h 3
103d 2
             2524-09-6   OfOfS-Triethylester
                         phosphorodithioic acid
(3.0 ± 0.2)E-5     l.OE-2
2.6y
             a.  Calculated ty the equation of Wolfe in Reference 18.

-------
                                                        P(OCH3)2
 (EtO)2P—O
O,O-Diethyl-O-pyrazinyl
    phosphorothioate
                                               O = S — N(CH3)2
        (EtO)2P
          (EtO)2P
                       Disulfoton
                        Phorate
                                             'CH,
         (MeO)2P
                              O
                       Dimethoate
.NH
                                          CH,
                 Figure 6. Phosphate Esters
                            34

-------
4.8  Alkylating Agents


     The four alkylating agents are all nitrogen mustards with  the


general structure I,
                    /C-C-Cl
                                                  c


             R	N:         	»-   R	-N	C
                    SC-C-C1                       C-C-Cl
                                                 II
where R is a substitutent that modifies reactivity.   The  rate


determining step in aqueous  solutions  is  formation of the highly


reactive ethyleneimmonium ion II.  The factor  of  five decrease  in


reactivity of chlornaphazine compared  to  cyclophosphamide is most


likely due to the delocalization of the free pair of  nitrogen


electrons over the phosphamide ring, slowing the  rate determining


formation of the ethyleneimonium ion  (Table 8,  Figure 7).


     Uracil mustard  (Figure  7) on  the  other hand  is approximately


three orders of magnitude more reactive than cyclophosphamide.
                                35

-------
                                                TABLE 8. AIKYIATING AGENTS
CAS Number
Ocxnpound
                                                  Rate Constants (25*0
 -4°id-i
M * hr *
Neutral
 hr"1
 -
M -  hr
Calculated  Ref.
Half-Life
pH 7, 25°C
66-75-1     Uracil mustard

305-03-3    Chlorantoucil

148-82-3    Melphalan

494-03-1    Qilornaphazine

50-18-0     cyclqphosphamide
                                    0.57 ± 0.08    (2.05 ± 0.2)E5    1.2h     2

                                        0.40                         l.Th     3

                                        0.15                       •  4.6h     3

                                       3.2E-3                        216h     3

                                       7.1E-4                         41d     3

-------
  Uracil Mustard
                     NH-
                               Melphalan
                                                    Chlorambucil
                                                      Cl
                                                     o
                                                     .NH
                                                                          Cl
                                                                           •H^O
Chlornaphazine
Cyclophosphamide
                       Figure?. AlkylatingAgents
                                    37

-------
4.9  Halogenated Ethers



     The halogenated ethers were discussed in the section on



bifunctional chloroalkanes (Section 4.2C).  The chloromethyl



ethers are orders of magnitude more reactive than ethers that have



two or more carbons interspersed between the chlorine and oxygen



(Table 9).  The 2-(2-chloroethoxy)ethanol is a product of



hydrolysis of bis-dichloroethyl ether but due to its larger



hydrolysis rate constant the concentration of 2-(2-chloroethoxy)



ethanol will remain low.
                                  38

-------
                                                              TABLE 9. HAIOGENATED ETHERS
Rate Constants f25°C) Calculated Ref .
CAS Number
107-30-2
111-44-4
628-89-7
Compound M hr
Chloronethyl methyl ether
bis-Dichloroethyl ether
2- (2-
-------
4.10 Oxidized Sulfur compounds
     The oxidized sulfur containing compounds in Table 10 are all
highly reactive.  It is of intrest that the hydrolysis rate
constants of the exo (Endosulfan I) and endo (Endosulfan II)
isomers of Endosulfan, for practical purposes,  are identical.
                                 40

-------
                                          TABLE 10. OXIDIZED SULFUR GCMPOUNDS
Rate Constants (25° C} Calculated Ref.
CAS Number Oonpound
Acid Neutral
M'1 hr"1 hr"1
Base Half-Life
M"1 hr"1 pH 7, 25eC
77-78-1     Dimethylsulfate                               0.6                       1.2 rain    10



1120-71-4   1,3-Eropane Sultone                           8.2E-2                      8.5h      3



959-98-8    Endosulfan I            (8.1 ± 2.7)E-3    (3.2 ± 2.0JE-3  (1.0 ± 0.7)E4   165h      2



33213-65-9  Endosulfan II           (7.4 ± 3.9)E-3    (3.7 ± 2.0)E-3  (1.5 ± 0.9)E4   133h      2



62-50-0     Ethyl metnanesulfonate                        1.5E-2                       46h      3

-------
                                   o
                                         O
                                   o
Cl
                         1,3-Propane Sultone
                                                                             S=0
  Endosulfan I
                                                    Endosulfan II
                     HC - S
                               O
 H

{-
 H
                           Ethyl methanesulfonate
                  Figure 8. Oxidized Sulfur Compounds
                                     42

-------
4.11 Other Miscellaneous Compounds



     The half-lives of the pyrophosphates and nitroso compounds in



Table 11 are so short, PRC discussions are meaningless.  Ethylene-



bis-(cithiocarbamic acid), 2,4-dithiobiuret, auramine, azaserine,



daunomycin, methylthiouracil, nitroglycerine, warfarin,



fluoroacetic acid sodium salt, and octamethylpyrophosphoramide



lack sufficient data for PRC discussion.  With the exception of a-



naphthylthiourea, thiourea and its substituted analogs are



resistant to hydrolysis.  Possibly the stability of the resulting



a-napthylamine enhances hydrolysis of a-napthylthiourea.  The rate



constants reported for chlorinated aromatics in part d of Table 2



make the reported hydrolysis rate constants for



pentachloronitrobenzene and /3-chloronaphthalene suspect.
                               43

-------
TABLE 11. MISCELLANEOUS COMPOUNDS
CAS Number
126-99-8
759-73-9
107-49-3
757-58-4
70-25-7
615-53-2
111-54-6
50-07-7
75-55-8
541-53-7
492-80-8
115-02-6
20830-81-3
86-88-4
82-68-8
56-84-2

-&**-!
Compound M ^ hr ^
2-Chloro-l , 3-butadiene
N-Nitroso-N-ethylurea
Tetraethyl pyrophosphate
Hexaethyl pyrophosphate
N-Methyl-N-riitro-N-nitrosoguaiiidine
N-Nitroso-N-methylurethane
Ethylene-bis (dithiocarbamic
acid) 848
Mitomycin C 4320
2-Methylaziridine
2 , 4-Dithiobiuret
Auramine
Azaserine 328 ± 20
Daunonycin
a-Naphthylthicurea
Pentacliloronitrobenzene
Methylthiouracil
Rate Constants ^25"
Neutral
hr'1
Polymerizes in
0.19
9.3E-2
9.3E-2
2.7E-2
2.9E-2
0.01
1.8E-3
8.0E-3
7.1 ± 1.3E-3
3.9E-4
2.6 ± 0.4E-4
9.7 ± 0.5E-5
8.0 ± 2.4E-5
2.8 ± 0.7E-5
9.7 ± 2.7E-6
C1 Calculated
Base Half-Life
M"1 hr"1 pH 7, 25°C
absence of inhibitors
5.3E6 0.96h
7.5h
7.5h
9.5E4 19h
2.9E3 24h
1 69h
4.30 12. 9d
87h
98h
74d
6.8 ± 0.7 99d
10 298d
9.9E2 361d
2.8y
8.2y
Ref.
3
3
3
3
3
3
3
22, 23
3
3
3
3
3
3
2
3

-------
                                                  TABLE 11.  MISCELLANEOUS OCMPCUNDS - continued
CAS Number
91-58-7
55-63-0
81-81-2
62-74-8
5344-82-1
62-56-6
152-16-9
96-45-7

-^-l
Compound M hr
0-Chloronaphthalene
Nitroglycerine
Warfarin 1.4E-4
FLuoroacetic acid,
sodium salt
1- (o-Cnlorophenyl) thiourea
Thiourea
Octamethylpyrophosphoramide 0.23 ± 0
Ethylene thiourea zero hydrolys
Pate Constants f25°C}
Neutral
hr"1
9.5 ± 2.8E-6

4.9E-6
<1.7E-6
(9.8 ± 3.0)E-7
<5.3E-7
.03
is within experimental
Cal c^il at*3^
Base Half-life
M'1 hr"1 pH 7, 25*C
8.3y
77 ± 11 lOy
0.026 16y
>47y
0.14 ± 0.03 81y
>150y
1E-4 3,400y
error after
Ref.
3
2
2
2
3
2
3
3
01
90 days at 90°C and pHs 3~, 7, and 11

-------
Predictive Techniques



     Table 12 contains second-order alkaline hydrolysis rate



constants that were either determined from laboratory measurements



(3, 11, 10, and 21), computer-estimated based on fundamental



molecular properties (9, SPARC) or correlation with infrared



spectra (8, Collette), or calculated using a simple regression



equation based on electronic and steric parameters (7).  Where



measured values were available for comparison, SPARC generally



predicted a higher value and Collette's correlation a lower value



but both were generally within a factor of two of the measured



value.



     The greater reactivity of methyl esters in comparison with



the corresponding ethyl esters is seen (Table 12) in the values



for three methyl-ethyl pairs.  SPARC lacked the parameters needed



to calculate a rate for the 2,4-D methyl ester containing the



phenoxy substituent.  A methyl substituent on the /3-carbon of a,/3-



unsaturated esters retards hydrolysis compared to a methyl on the



a-carbon.  The )8-carbon methyl apparently strengthens the



inductive IT electron resonance with the carbonyl carbon and



retards attack by the negatively charged hydroxyl ion.  Steric



hindrance by the methyl on the a-carbon is not a factor due to the



planar orientation of substituents on the double bond.



     Figure 9 is a SPARC-generated pH-rate profile for methyl



methacylate.  This allows calculation of \ at any pH.
                                 46

-------
  TABLE 12. PREDICTED AND lABORATORY DETERMINED HYDROLYSIS RATE CONSTANTS OF CARBOXYIATE ESTERS
CAS Number
80-62-6



96-33-3





93-89-0

1928-38-7

Compound
Methyl methacrylatea


Ethyl methacrylate
Methyl acrylate
Ethyl acrylate
trans-Ethyl crotonate0'


trans-Methyl crotonate
Ethyl benzoate

2,4-D-Methyl ester

Rate Constants (25' a
Acid Neutral Base
M"1 hr'1 hr'1 M"1 hr'1
200 ± 47b
279
70
185
408b
21013
47"
86
10.9
207
108b
134
41,000 ± 5,000**
26,080
Calculated
Half-Life
pH 7, 25°C
3.9y
2.8y
n.3y
4.3y
l.9y
3.8y
16. 8y
9.2y
72y
3.8y
7.3y
5.9y
7d
lid
Ref.
3
9*
8**
9*
11
11
21
9*
_***
9*
10
9*
4
8**
a.  Methyl 2-methylacrylate.
b.  Determined in the laboratory.
c.  Ethyl 3-methylacrylate
d.  Halonen also reported an identical rate for the cis isomer.
  * SPARC
 ** Collette
*** Drossman et al

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     -2
pH  Profile  methyl  methacrylate
   &

   D>
   O
     -9
                                         8
                                   PH
Figure 9.  SPARC Generated pH-rate Profile of Methyl Methacrylate
                             48

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                            References

      1.  Arcos, J.C.  1988.  Structure-Activity Relationships.
Environ. Sci. Technol.  21f 743-745.

      2.  Ellington, J.J., F.E. Stancil, Jr., and W.D. Payne.
1987.  Measurements of Hydrolysis Rate Constants for Evaluation of
Hazardous Waste Land Disposal: Volume I.  Data on 32 Chemicals.
U.S. Environmental Protection Agency, Athens, GA.  EPA/600/3-
86/043.

      3.  Ellington, J.J., F.E. Stancil, Jr., W.D. Payne, and C.D.
Trusty.  1987-  Measurement of Hydrolysis Rate Constants for
Evaluation of Hazardous Waste Land Disposal: Volume II.  Data on
54 Chemicals.  U.S. Environmental Protection Agency, Athens, GA.
EPA/600/3-87/019.

      4.  Ellington, J.J., F.E. Stancil, Jr., W.D. Payne, and C.D.
Trusty.  1988.  Measurement of Hydrolysis Rate Constants for
Evaluation on Hazardous Waste Land Disposal: Volume III.  Data on
70 Chemicals.  U.S. Environmental Protection Agency, Athens, GA.
EPA/600/3-88/028.

      5.  Ellington, J.J., F.E. Stancil, Jr., W.D. Payne, and C.D.
Trusty.  1988.  Interim Protocols for Measuring Hydrolysis Rate
Constants in Aqueous Solutions.  U.S. Environmental Protection
Agency, Athens, GA.  EPA/600/3-88/014.

      6.  Shorter, J.  1973.  Correlation Analysis in Organic
Chemistry, Claredon Press: Oxford.

      7-  Drossman, H., H. Johnson, and T. Mill.  1988.  Structure
Activity Relationships for Environmental Processes 1: Hydrolysis
of Esters and Carbamates.  Chemosphere.  17. 1509-1530.

      8.  Collette, T.W.  1989.  The Potential for Predicting
Process Constants with Spectroscopic Data, 19th International
Symposium on Environmental Analytical Chemistry/ Jekyll Island,
GA.

      9.  Karickhoff, S.W., L.A. Carreira, C. Melton, V.K.
McDaniel, A.N. Vellino, and D.E. Nute.  1989.  Predicting Chemical
Reactivity by Computer, Part I: Approach.  Submitted  for
publication.

     10.  Mabey, W. and T. Mill.  1978.  Critical Review of
Hydrolysis of Organic Compounds in Water Under Environmental
Conditions.  J. Phys. Chem. Ref. Data.  7(2):383-415.

     11.  Sharma, R.C. and M.M. Sharma.  1970.  Kinetics of
Alkaline Hydrolysis of Esters.  II Unsaturated Esters and Oxalic
Esters.  Bull. Chem. Soc.  Japan.  43.  642-645.
                                 49

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     12.  Jeffers, P.M., L.M. Ward, L.M. Woytowitch, and N.L.
Wolfe.  1989.  Homogeneous Hydrolysis Rate Constants for Selected
Chlorinated Methanes, Ethanes, Ethenes and Propanes.  In press
Environmental Science and Technology.

     13.  Queen, A. and R.E. Robertson.  1966.  Heat Capacity of
Activation for the Hydrolysis of 2,2-Dihalopropanes.  J. Am. Chem.
Soc.  88./ 1363-1365.

     14.  Jungclaus, G.A. and S.Z. Cohen.  1986.  Extended
Abstracts, 191st National Meeting of the American  Chemical
Society, Division of Environmental Chemistry, New York, NY;
American Chemical Society: Washington, DC, 1986: paper 6.

     15.  Jeffers, P.W.  1989.  Private Communication.

     16.  Metwally, M., El-Sayed, and N.L. Wolfe.  1989.
Hydrolysis of Chlorosilbene Oxide.  Submitted for publication.

     17.  Cox, J.R. and O.B. Ramsay.  1964.  Mechanisms of
Substitution in Phosphate Esters.  Chem. Rev. 64. 317-352.

     18.  Wolfe, N.L.  1981.  Organophosphate and
Organophosphorothioate Esters:  Application of Linear Free Energy
Relationships to Estimate Hydrolysis Rate Constants for Use in
Environmental Fate Assessment.  Chemosphere 9_, 571-579.

     19.  Perrin, D.D., B. Demsey, and E.P. Serjeant.  1981.  pKa
Prediction for Organic Acids and Bases.  Chapman  and Hall, New
York, NY.

     20.  VanDuuren, B.L., C. Katz, B.M. Goldschmidt, K. Frenkel,
and A. Sivak.  1972.  Carcinogeniety of Halo-esters.  II
Structure-Activity Relationships of Analogs of bis(Chloromethyl)
ether.  J. Nat. Cancer Inst.  48. 1431-1439.

     21.  Halonen, E.A.  1955.  The Effect of Substituents and
a,/3-Unsaturation on the Alkaline Hydrolysis of a,/J-Unsaturated
Aliphatic Esters.  Acta Chem. Scand.  9. 1492-1497.

     22.  McClelland, R.A. and K. Lam.  1985.  Kinetics and
Mechanism of the Acid Hydrolysis of Mitomycins.   J. Am. Chem. Soc.
107. 5182-5186.

     23.  Beijnen, J.H., J. Den Hartigh, and W.J.M. Underberg.
1985.  Quantitative Aspects of the Degradation of Mitomycin C in
Alkaline Solution.  J. Pharm. Biomed. Anal. 3_, 59-69.
                                50

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* ••  H  UNITED STATES ENVIRONMENTAL PROTECTION AGENCY
                         WASHINGTON. D.C. 20460
                                                       OFFICE OF
                                                 RESEARCH AND DEVELOPMENT
   SUBJECT:   Transmittal  of  ORD  Project  Report  Entitled  Hydrolysis
             Rate  Constants  for  Enhancing  Property-Reactivity
            .Relationships  (DeJ4xjer,abfhe0 7950A)y

   FROM:   /^Courtney  Riordan        _
          7   Director,  Office^of^Environmental  Processes
                and  Effects  Research  (RD-682)

   TO:        Sylvia  Lowrance
             Director,  Office  of Solid Waste  (OS-300)

       The  attached copy of the subject ORD  project  report  is  being
   delivered  to  your office  in response  to the  Agency's  need  ro
   accurate  hydrolysis  rate  constants  foruse  in mathematical  models
   for  predicting  chemical movement  form hazardous  waste  sites  and
   other  pollution  sources.   The document  has  been  subjected  to the
   Agency's  peer and administrative  review, and will  be  published as
   an EPA  report.

       A  major  objective of this  work was to  establish  new,  or
   expand  existing,  property-reactivity  correlations  by  examining
   rate constants  for  hydrolysis in  water  of  10 classes  of organic
   compounds.  Such  correlations can  then  be  used  to  predict
   environmental hydrolysis  fate of  chemicals  that  have  similar
   molecular  structure.

       The  compound classes covered  by  this  report include
   aliphatic  and aromatic carboxylate  esters,  alkyl and  aromatic
   halides,  amides,  carbamates,  epoxides,  nitriles, phosphate
   esters, alkylating  agents,  halogenated  ethers,  and  oxidized
   sulfur  compounds.   Three  predictive techniques  (one  based  on
   empirical  correlation  with  derived  constants,  the  second  based on
   infrared  spectra,  and  the third based on fundamental  calculations
   required  only chemical structure)  were  used  and  compared  for the
   predicted  rate  constants  were generally within  a factor of  two of
   each other  and  the  laboratory-determined values.

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     This document is a product of the Land Disposal Assessment
and Evaluation of Other Management Systems research program at
the Environmental Research Laboratory-Athens.   Dr.  Zubair Saleem
of your Characterization and Assessment Division  is familiar
with and has been an active contributor to the project's results.

Attachment

cc:  Elizabeth Bryan (TS-798)

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