FIELD: chemistry.
SUBSTANCE: present invention relates to a method of producing 2-amino-nicotinic acid benzyl ester derivative. Method of producing 2-amino-nicotinic acid benzyl ester involves reacting 2-amino-nicotinic acid derivative of the following formula [I], in which R1 means a hydrogen atom or C1-C4 alkyl group and M is a hydrogen atom or an alkali metal, with a benzyl derivative of the following formula [II], in which R2 means a hydrogen atom, a halogen atom, C1-C4 alkyl group or C1-C4 alkoxy group, A is a nitrogen atom or a methine group (CH), X is a hydroxy group or a halogen atom, and Y is an oxygen atom, a methylene group (CH2) or methyleneoxy group (OCH2), (a) using a base, where M denotes a hydrogen atom in formula [I], and (b) using a halogenating reagent, where X denotes a hydroxy group in formula [II], and then reacting 2-amino-nicotinic acid derivative with a benzyl derivative in an aromatic hydrocarbon solvent in the presence of an interphase catalyst or a tertiary amine to obtain 2-amino-nicotinic acid benzyl ester, described by the following formula [III], in which R1, R2, A and Y are as defined for formulas [I] and [II]. Also disclosed are versions of a method of producing 2-amino-nicotinic acid benzyl ester.
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EFFECT: obtaining 2-amino-nicotinic acid benzyl ester derivative with high output at high purity, with high volumetric efficiency.
3 cl, 1 tbl, 5 ex
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