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Patent Searching and Data


Title:
GREEN SYNTHESIS PROCESS FOR PREPARING PERINDOPRIL TERT-BUTYLAMINE SALT
Document Type and Number:
WIPO Patent Application WO/2018/191999
Kind Code:
A1
Abstract:
The present invention relates to a process for preparing perindopril, the process mainly involving oxidizing ethyl 3-ketohexanoate as a raw material to synthesize ethyl 2-ketovalerate, then subjecting same to condensation ammoniation and catalytic asymmetric hydrogenation with methyl L-alaninate hydrochloride having an asymmetric optical activity to obtain a methyl N-[(S)-ethoxycarbonylbutyl]-(S)-alaninate intermediate having an asymmetric optical activity, directly subjecting the latter to amidation with (2S,3S,7S)-octahydroindole-2-carboxylic acid under the catalysis of a Lewis acid to obtain a perindopril product having an asymmetric optical activity, and then salifying same with tert-butylamine to obtain an amorphous perindopril tert-butylamine salt crystal for medical use. The synthesis process has a simple method, mild conditions, a high yield and a low cost, and is a new green synthesis process for preparing perindopril tert-butylamine salt.

Inventors:
WANG XIAOMING (CN)
ZHOU YABING (CN)
DING WENMING (CN)
GU PEI (CN)
ZHU YUN (CN)
Application Number:
CN2017/082095
Publication Date:
October 25, 2018
Filing Date:
April 27, 2017
Export Citation:
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Assignee:
SHANGHAI PHARMA DONGYING JIANGSU PHARMACEUTICAL CO LTD (CN)
International Classes:
C07K5/062; C07C227/32; C07D209/00
Foreign References:
EP1675827B12009-12-16
CN1176903C2004-11-24
Other References:
YANG, XINHUA: "Synthesis of Perindopril Erbumine", CHEMICAL WORLD, 25 September 2010 (2010-09-25), pages 552 - 554
STERGIOU, A. ET AL.: "Oxone-Mediated Oxidative Cleavage of beta-Keto, Esters and 1, 3-Diketones to a-Keto Esters and 1, 2-Diketones in Aqueous Medium", J. ORG. CHEM., vol. 78, no. 14, 19 July 2013 (2013-07-19), pages 7268 - 7273, XP055545031
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