公开(公告)号：EP4201926A1

公开(公告)日：2023-06-28

申请号：EP21905250.3

申请日：2021-10-13

申请人： Sichuan University

发明人： QIN, Yong ,  XUE, Fei ,  SONG, Hao ,  LIU, Xiaoyu ,  ZHANG, Dan ,  HE, Huan

IPC分类号： C07D221/28 ,  C07D489/08

摘要： The present application relates to the field of drug synthesis, in particular to a novel intermediate, a method for preparing the same and application thereof. The structural formula of the novel intermediate provided by the present application is as expressed by formula I:

where R is a secondary amine protection group. Based on the possible biogenic pathway of morphine derivatives, the present application realizes the efficient synthesis of morphine derivatives through the strategy of biomimetic synthesis, taking the asymmetric transfer hydrogenation reaction and the intramolecular oxidative dearomatization Heck reaction in the process of preparing the intermediate as the key reactions of total synthesis. Using the novel intermediate provided by the present application to synthesize morphine derivatives has the characteristics of significantly reducing the synthesis steps, improving the yield, reducing the discharge of three wastes and reducing the production cost.

公开(公告)号：EP4183792A1

公开(公告)日：2023-05-24

申请号：EP20944871.1

申请日：2020-07-14

申请人： Sichuan University ,  Academy of Military Medical Sciences

发明人： LIU, Xiaoyu ,  QIN, Yong ,  ZHONG, Wu ,  CAO, Ruiyuan ,  HE, Huan ,  ZHENG, Zhibing ,  LI, Song

IPC分类号： C07H5/06 ,  C07H1/00 ,  C12P19/26 ,  C12P19/44 ,  A61K31/70 ,  A61P31/00

摘要： The invention relates to a compound represented by general Formula I, a stereoisomer thereof, a pharmaceutically acceptable salt thereof, a pharmaceutically acceptable ester thereof, a pharmaceutically acceptable hydrate thereof or pharmaceutically acceptable solvate thereof, and the invention also relates to a pharmaceutical composition comprising the compound, and a preparation method for the compound and a use of the compound.