The application relates to a process for the synthesis of organic sulfonic acid salts of amino acid esters comprising the steps of (i) reacting at least one lactam with at least 3 carbon atoms in the lactam ring with at least one organic sulfonic acid in an aqueous solution, (ii) esterification of the organic sulfonic amino acid salt of step (i) with at least one alcohol with at least 8 carbon atoms comprising at least one hydroxyl group, (iii) optionally removal of water and/or removal of excess alcohol of step (ii). The application also relates to organic sulfonic acid salts of amino acid esters of the general formula (I).

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A process to prepare an amine-functional ester of an amino carboxylic acid includes the step of reacting a polyol of the formula (I)

HO-A-OH  (I)

where A is a carbon chain with about 2 to about 36 carbon atoms that is aliphatic linear or branched, saturated or unsaturated, or aromatic, or CH.sub.2CH(OH)CH.sub.2, CH.sub.2C(CH.sub.2OH).sub.2CH.sub.2, CH.sub.2C(CH.sub.2OH)(CH.sub.3)CH.sub.2, CH.sub.2C(CH.sub.2OH)(CH.sub.2CH.sub.3)CH.sub.2, p-tetrahydrofuran, erythritol or an ester of di- or tricarboxylic acids with ethylene or propylene glycol, and wherein A can optionally be alkoxylated or reacted with hydroxy carboxylic acids, with an aminocarboxylic acid of formula II or its cyclic amide of the formula III, where m is an integer of about 1 to about 8 in formula II and about 3 to about 8 in formula III, each R independently is hydrogen or a C1-C4 alkyl group, or CH.sub.2CH.sub.2COOH, or CH.sub.2COOH, or (CH.sub.2).sub.4NH.sub.2, in the presence of a Brønsted-Lowry acid.

A process to prepare an amine-functional ester of an amino carboxylic acid includes the step of reacting a polyol of the formula (I)

HO-A-OH  (I)

where A is a carbon chain with about 2 to about 36 carbon atoms that is aliphatic linear or branched, saturated or unsaturated, or aromatic, or CH.sub.2CH(OH)CH.sub.2, CH.sub.2C(CH.sub.2OH).sub.2CH.sub.2, CH.sub.2C(CH.sub.2OH)(CH.sub.3)CH.sub.2, CH.sub.2C(CH.sub.2OH)(CH.sub.2CH.sub.3)CH.sub.2, p-tetrahydrofuran, erythritol or an ester of di- or tricarboxylic acids with ethylene or propylene glycol, and wherein A can optionally be alkoxylated or reacted with hydroxy carboxylic acids, with an aminocarboxylic acid of formula II or its cyclic amide of the formula III, where m is an integer of about 1 to about 8 in formula II and about 3 to about 8 in formula III, each R independently is hydrogen or a C1-C4 alkyl group, or CH.sub.2CH.sub.2COOH, or CH.sub.2COOH, or (CH.sub.2).sub.4NH.sub.2, in the presence of a Brønsted-Lowry acid.

A process to prepare an amine-functional ester of an amino carboxylic acid includes the step of reacting a polyol of the formula (I)

HO-A-OH  (I)

where A is a carbon chain with about 2 to about 36 carbon atoms that is aliphatic linear or branched, saturated or unsaturated, or aromatic, or CH.sub.2CH(OH)CH.sub.2, CH.sub.2C(CH.sub.2OH).sub.2CH.sub.2, CH.sub.2C(CH.sub.2OH)(CH.sub.3)CH.sub.2, CH.sub.2C(CH.sub.2OH)(CH.sub.2CH.sub.3)CH.sub.2, p-tetrahydrofuran, erythritol or an ester of di- or tricarboxylic acids with ethylene or propylene glycol, and wherein A can optionally be alkoxylated or reacted with hydroxy carboxylic acids, with an aminocarboxylic acid of formula II or its cyclic amide of the formula III, where m is an integer of about 1 to about 8 in formula II and about 3 to about 8 in formula III, each R independently is hydrogen or a C1-C4 alkyl group, or CH.sub.2CH.sub.2COOH, or CH.sub.2COOH, or (CH.sub.2).sub.4NH.sub.2, in the presence of a Brønsted-Lowry acid.

The present disclosure relates to a process to prepare esters of an amino carboxylic acid of the formula (I) comprising the steps of reacting an aminocarboxylic acid present as a cyclic amide of the formula II and an alkanol of the formula R—(O-A)mOH in the presence of the Brønsted-Lowry acid at a temperature of between about 60 and about 200 degrees C. wherein the total molar amount of aminocarboxylic acid to the molar amount of the alkanol is between about 1:0.8 and about 1:1.5 and wherein the Brønsted-Lowry acid is not added to the reaction mixture until least about 50% of the total of the alkanol and cyclic amide are added to the reaction mixture.

The present disclosure relates to a process to prepare esters of an amino carboxylic acid of the formula (I) comprising the steps of reacting an aminocarboxylic acid present as a cyclic amide of the formula II and an alkanol of the formula R—(O-A)mOH in the presence of the Brønsted-Lowry acid at a temperature of between about 60 and about 200 degrees C. wherein the total molar amount of aminocarboxylic acid to the molar amount of the alkanol is between about 1:0.8 and about 1:1.5 and wherein the Brønsted-Lowry acid is not added to the reaction mixture until least about 50% of the total of the alkanol and cyclic amide are added to the reaction mixture.

The present disclosure relates to a process to prepare esters of an amino carboxylic acid of the formula (I) comprising the steps of reacting an aminocarboxylic acid present as a cyclic amide of the formula II and an alkanol of the formula R—(O-A)mOH in the presence of the Brønsted-Lowry acid at a temperature of between about 60 and about 200 degrees C. wherein the total molar amount of aminocarboxylic acid to the molar amount of the alkanol is between about 1:0.8 and about 1:1.5 and wherein the Brønsted-Lowry acid is not added to the reaction mixture until least about 50% of the total of the alkanol and cyclic amide are added to the reaction mixture.

Disclosed herein are embodiments of a compound that inhibits c-Abl tyrosine kinase (also referred to herein as “c-Abl”). The compound embodiments described herein are novel c-Abl inhibitors that can bind to c-Abl at an allosteric site and inhibit its activity in various pathways. The compound embodiments also are capable of crossing the blood brain barrier and therefore are useful in inhibiting c-Abl activity as it affects pathways and/or proteins in the brain. The compound embodiments described herein are effective therapeutic agents for treating diseases involving c-Abl, such as cancers, motor neuron diseases, and neurodegenerative diseases. Also disclosed herein are embodiments of methods for making and using the c-Abl inhibitory compound embodiments.

Disclosed herein are embodiments of a compound that inhibits c-Abl tyrosine kinase (also referred to herein as “c-Abl”). The compound embodiments described herein are novel c-Abl inhibitors that can bind to c-Abl at an allosteric site and inhibit its activity in various pathways. The compound embodiments also are capable of crossing the blood brain barrier and therefore are useful in inhibiting c-Abl activity as it affects pathways and/or proteins in the brain. The compound embodiments described herein are effective therapeutic agents for treating diseases involving c-Abl, such as cancers, motor neuron diseases, and neurodegenerative diseases. Also disclosed herein are embodiments of methods for making and using the c-Abl inhibitory compound embodiments.

The present invention relates to a method for preparing pregabalin by a biological enzyme method. In particular, the method comprises producing pregabalin B and an R-configuration compound C by using a compound A as a raw material under the action of a biological enzyme; performing configuration inversion of the separated and recovered R-configuration compound C under the action of an isomerase to produce an S-configuration compound D; and producing pregabalin B from the compound D under the action of a biological enzyme

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