Title: Process for synthesising enalapril
Application Number: 85105258 Application Date: 1985.07.04
Publication Number: 1006285 Publication Date: 1986.12.31
Approval Pub. Date: Granted Pub. Date: 1989.10.18
International Classifi-cation: A61K37/02,C07K5/06
Applicant(s) Name: Shanghai Medical Industrial Inst., State Medical M Address:
Inventor(s) Name: Chen Guangyan, Shi Huiling
Attorney & Agent:
Abstract:
     Enalapril is a newly developed blood vessel tension swivelase inhibitor. Its carative effect for various type of hypertensions is notable in clinic and it is also used for curing congestional heart failure. In the synthesis process, by reducing and ammoniating ethyl ester of alpha-phenyl-butanone acid and benzyl alanine, or by catalytically hydrogenating after condensing ethyl ester of alpha-Bromophenyl butyric acid and benzyl alanine, N-(1-S-carbethoxyl group)-phenepropyl-alanine is prepared. Then, it and N-hydroxy-succinimide are condensed under the action of DCC to obtain activating ester. After that, enalapril is prepared by condensing activating ester and proline-hydroxy-tetramethyl-ammonium. With this method, we can avoid using protective group and highly toxic benzyl chloroformate and tertiary butyrolactone chloroformate.
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