公开(公告)号：EP4438592A1

公开(公告)日：2024-10-02

申请号：EP22964190.7

申请日：2022-11-21

申请人： Shanghai Bios Technology Co., Ltd.

发明人： YU, Wansheng ,  RUAN, Libo ,  PENG, Qiujun ,  ZENG, Yifei

IPC分类号： C07C271/22 ,  C07C269/00 ,  C07C247/16 ,  C12P13/02 ,  C07D307/00

CPC分类号： Y02P20/55

摘要： The present invention discloses an edoxaban intermediate, and a preparation method therefor. A general structural formula of the edoxaban intermediate is

or

wherein R1 is OH, alkoxy or a N,N-dialkyl group, and R2 is hydrogen, alkoxycarbonyl or an amino protecting group. The preparation method includes subj ecting

and an oxidizing agent to an oxidation reaction to obtain a compound of a formula II; and mixing the compound of the formula II, an aminotransferase, an aminotransferase coenzyme, and a phosphate buffer solution for an enzyme catalyzed reaction or further amine derivatization to obtain a compound of a formula I. Compared with chemical synthesis methods in the prior art, such key edoxaban intermediates and the preparation method therefor provided by the present invention have the advantages of a novel structure, mild reaction conditions, and high yield, having good industrial values.

公开(公告)号：EP4438595A1

公开(公告)日：2024-10-02

申请号：EP22966354.7

申请日：2022-12-09

申请人： Shanghai Bios Technology Co., Ltd.

发明人： PENG, Qiujun ,  YU, Wansheng ,  RUAN, Libo ,  ZENG, Yifei ,  LI, Qinqin

IPC分类号： C07D213/75 ,  C07D513/04

CPC分类号： Y02P20/55 ,  C07D513/04 ,  C07D213/75

摘要： The present invention discloses an edoxaban key intermediate and a synthesis method therefor. The edoxaban key intermediate is

and is prepared by an ammonolysis reaction between raw materials. Edoxaban p-toluenesulfonate monohydrate can be prepared by using this intermediate. Edoxaban p-toluenesulfonate hydrate is prepared on an industrial scale by using a new method and a new route which are simple and efficient and can effectively reduce the cost.