公开(公告)号：EP4450508A1

公开(公告)日：2024-10-23

申请号：EP21967736.6

申请日：2021-12-17

申请人： Zhejiang Jiuzhou Pharmaceutical Co., Ltd.

发明人： MEI, Yijiang ,  LIU, Shengmin ,  LI, Yonggang ,  FAN, Jinmin ,  HU, Kai ,  GAO, Shizhao

IPC分类号： C07D513/04 ,  C07D211/74

摘要： Disclosed are an intermediate of edoxaban tosylate and a preparation method therefor, having the advantages that the preparation process is simple, reaction conditions are mild, the cost is low, and raw materials are easily to be obtained. The method comprises the synthesis steps of: substitution reaction, thiolation reaction, cyclization reaction, esterification reaction with alcohol to obtain a compound represented by formula (V), and then reacting to obtain a compound represented by formula (VI), or directly reacting the compound represented by formula (IV) under the effect of alcohol and acid, to obtain the compound represented by formula (VI), and subjecting the compound represented by formula (VI) to alkali hydrolysis and acid neutralization to obtain a compound represented by formula (VII). The reaction formula is as follows:

公开(公告)号：EP4008712A1

公开(公告)日：2022-06-08

申请号：EP20848133.3

申请日：2020-06-08

申请人： Zhejiang Jiuzhou Pharmaceutical Co., Ltd

发明人： LI, Hongliang ,  ZHANG, Xianyi ,  GAO, Zhaobo ,  MEI, Yijiang

IPC分类号： C07C227/36 ,  C07C231/12 ,  C07D241/08 ,  C07D295/185 ,  C07D471/04 ,  C07D487/04 ,  C07C229/34 ,  C07C233/47 ,  C07C229/12 ,  C07C229/18 ,  C07B55/00

摘要： The present disclosure relates to the field of medicine synthesis, and relates to a method for a racemic preparation of chiral β -amino acids and derivatives thereof, and in particular to a method for racemizing sitagliptin intermediates.

where R 1 is hydrogen, alkyl or aryl; R 2 is hydrogen, alkyl or aryl; R 3 is hydrogen, alkyl, aryl or acyl; R 4 is alkyl, aryl, OR', SR', NHR' or NR'R", wherein R', R" are hydrogen, alkyl or aryl.