Title:
METHOD FOR SYNTHESIZING DILTIAZEM HYDROCHLORIDE AND USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2022/257288
Kind Code:
A1
Abstract:
The present invention belongs to the field of drug synthesis, and discloses a method for synthesizing diltiazem hydrochloride and the use thereof. The method for synthesizing diltiazem hydrochloride provided by the present invention comprises: carrying out a ring-closing condensation reaction and an esterification reaction on cis-(2S,3S) compound 1 and compound 2, and then adding hydrochloric acid to form a salt, namely diltiazem hydrochloride. The method for synthesizing diltiazem hydrochloride provided by the present invention reduces the synthetic steps, improves the reaction yield, reduces the industrial production cost, and reduces the time cost of synthesis. The present invention is applicable to the synthesis of diltiazem hydrochloride, and the synthesized diltiazem hydrochloride is used for preparing diltiazem hydrochloride for injection.
Inventors:
PAN SHUHUA (CN)
WANG JINYU (CN)
WANG SHOUCHUN (CN)
WANG JINYU (CN)
WANG SHOUCHUN (CN)
Application Number:
PCT/CN2021/118177
Publication Date:
December 15, 2022
Filing Date:
September 14, 2021
Export Citation:
Assignee:
HAINAN JIN RUI PHARMACEUTICAL CO LTD (CN)
International Classes:
C07D281/10; A61K9/00; A61K31/554; A61P9/00; A61P9/10
Foreign References:
| CN113336724A | 2021-09-03 | |||
| JPS62187427A | 1987-08-15 | |||
| CN110407771A | 2019-11-05 | |||
| CN110407770A | 2019-11-05 | |||
| CN110642874A | 2020-01-03 | |||
| CN101443014A | 2009-05-27 |
Other References:
WATSON KEITH G., FUNG YIK M., GREDLEY MATTHEW, BIRD GRAHAM J., JACKSON W. ROY, GOUNTZOS HELEN, MATTHEWS BARRY R.: "Asymmetric syntheses of (+)-diltiazem hydrochloride", JOURNAL OF THE CHEMICAL SOCIETY, CHEMICAL COMMUNICATIONS, no. 15, 1 January 1990 (1990-01-01), GB , pages 1018 - 1019, XP093012704, ISSN: 0022-4936, DOI: 10.1039/c39900001018
Attorney, Agent or Firm:
BEIJING HC-IP AGENCY CO., LTD. (GENERAL PARTNERSHIP) (CN)
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