Title:
METHOD FOR PREPARING ROXATIDINEACETATEHYDROCHLORIDE AND INTERMEDIATE THEREOF
Document Type and Number:
WIPO Patent Application WO/2019/075976
Kind Code:
A1
Abstract:
Disclosed is a method for preparing roxatidineacetatehydrochloride and an intermediate thereof, comprising the following steps: dissolving m-hydroxybenzaldehyde in a solvent, dropping piperidine into the solution, adding sodium borohydride, and then carrying out post-treatment to prepare 3-(1-piperidinyl methyl)phenol; adding a standby solution of 3-chloropropylamine hydrochloride into 3-(1-piperidinyl methyl)phenol to prepare an intermediate, i.e., 3-[3-(1-piperidinyl methyl) phenoxyl] propylamine; and after the reaction is ended, adding acetoxyacetyl chloride to perform reaction so as to prepare a final product, i.e., roxatidineacetatehydrochloride. The present method for preparing roxatidineacetatehydrochloride and an intermediate thereof can achieve stable yield and quality, enables the quality to be controllable, is environmentally friendly, has low costs, and facilitates industrial production.
Inventors:
ZHANG YANG (CN)
ZHAO ZHENGANG (CN)
CHENG XIAOFENG (CN)
CHI KAIYUE (CN)
ZHAO ZHENGANG (CN)
CHENG XIAOFENG (CN)
CHI KAIYUE (CN)
Application Number:
PCT/CN2018/077035
Publication Date:
April 25, 2019
Filing Date:
February 23, 2018
Export Citation:
Assignee:
BEIJING AOHE DRUG RES INSTITUTE CO LTD (CN)
SIHUAN PHARMACEUTICAL HOLDINGS GROUP LTD (CN)
SIHUAN PHARMACEUTICAL HOLDINGS GROUP LTD (CN)
International Classes:
C07D295/096
Foreign References:
| CN102993121A | 2013-03-27 | |||
| CN101717363A | 2010-06-02 | |||
| CN1986535A | 2007-06-27 | |||
| EP0559190A1 | 1993-09-08 | |||
| CN107857743A | 2018-03-30 |
Attorney, Agent or Firm:
BEIJING LINKAW PATENT ATTORNEY LAW FIRM (CN)
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