公开(公告)号：US20230348412A1

公开(公告)日：2023-11-02

申请号：US18000099

申请日：2021-05-26

申请人： Hangzhou Zhongmei Huadong Pharmaceutical Co., Ltd.

发明人： Fan HU ,  Yubao ZHOU ,  Li FANG ,  Haiwen HU ,  Zhongjun XU

IPC分类号： C07D319/16 ,  C07D491/056

CPC分类号： C07D319/16 ,  C07D491/056

摘要： The present invention relates to a method for preparing GLP-1 receptor agonist, specifically relates to an industrialized method for preparing a GLP-1 receptor agonist (S)-2-(3S,8S)-3-(4-(3,4-dichlorobenzyloxy)phenyl-7-((S)-1-phenylpropyl)-2,3,6,7,8,9-hexahydro-[1,4]-dioxino[2,3-g]isoquinolin-8-ylformylamino)-3-(4-(2,3-dimethylpyridin-4-yl)phenyl)propanoic acid dihydrochloride (compound I). The method utilizes compound 1 as the starting material, which undergoes nucleophilic addition, hydrolysis, reduction ammoniation, cyclization, amide condensation, hydrolysis, and salt forming reaction to give compound I. The method for preparing compound I has a total yield of more than 35%, with purity of compound I more than 98%.