A NEW PROCESS FOR THE PREPARATION OF LERCANIDIPINE HYDROCHLORIDE

A NEW PROCESS FOR THE PREPARATION OF LERCANIDIPINE HYDROCHLORIDE

A process for preparing lercanidipine hydrochloride is provided, thereby improving yield by performing the process under mild condition in the presence of a coupling reagent, simplifying the process, and easily removing a by-product using water, so that the lercanidipine hydrochloride can be simply...

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Hauptverfasser: SUH, JUNG JIN, CHOI, JANG SIK, PARK, CHANG KWON
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CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
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creator SUH, JUNG JIN
CHOI, JANG SIK
PARK, CHANG KWON
description A process for preparing lercanidipine hydrochloride is provided, thereby improving yield by performing the process under mild condition in the presence of a coupling reagent, simplifying the process, and easily removing a by-product using water, so that the lercanidipine hydrochloride can be simply and stably mass produced. The process for preparing lercanidipine hydrochloride represented by formula (1) comprises reacting 2,6-dimethyl-5- methoxycarbonyl-4- (3-nitrophenyl)- 1,4-dihydropyridine- 3-carboxylic acid of formula (2) with 2,N-dimethyl-N- (3,3-diphenylpropyl)- 1-amino-2-propanol of formula (3) in the presence of 2-chloro-1,3-dimethylimidazolium chloride of formula (4) as a coupling reagent and base in solvent at 10 to 60 deg. C, wherein the solvent is selected from dichloromethane, 1,2-dichloroethane and chloroform; and the base is pyridine, trimethylamine and triethylamine.
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The process for preparing lercanidipine hydrochloride represented by formula (1) comprises reacting 2,6-dimethyl-5- methoxycarbonyl-4- (3-nitrophenyl)- 1,4-dihydropyridine- 3-carboxylic acid of formula (2) with 2,N-dimethyl-N- (3,3-diphenylpropyl)- 1-amino-2-propanol of formula (3) in the presence of 2-chloro-1,3-dimethylimidazolium chloride of formula (4) as a coupling reagent and base in solvent at 10 to 60 deg. 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HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
title A NEW PROCESS FOR THE PREPARATION OF LERCANIDIPINE HYDROCHLORIDE
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