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专利概况
专利名称 METHOD FOR PREPARING ROXATIDINEACETATEHYDROCHLORIDE AND INTERMEDIATE THEREOF
申请号 WOCN18077035 申请日
公开(公告)号 WO2019075976A1 公开(公告)日
申请(专利权)人 BEIJING AOHE DRUG RESEARCH INSTITUTE CO LTD; SIHUAN PHARMACEUTICAL HOLDINGS GROUP LTD 发明人 ZHANG Yang; ZHAO Zhengang; CHENG Xiaofeng; CHI Kaiyue
专利来源 国家知识产权局 转化方式
摘要

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.

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