公开(公告)号：EP4186915A1

公开(公告)日：2023-05-31

申请号：EP21841411.8

申请日：2021-07-15

申请人： Sichuan University ,  Academy of Military Medical Sciences ,  Chengdu Aupone Pharmaceutical Co., Ltd.

发明人： QIN, Yong ,  ZHONG, Wu ,  XUE, Fei ,  LIU, Xiaoyu ,  WANG, Yu ,  ZHOU, Xiaohan ,  LIU, Bo ,  WANG, Ke ,  YANG, Likai ,  ZHOU, Ruijie ,  XIAO, Yaxin ,  XUE, Fanglin ,  ZHANG, Minjie ,  SONG, Hao ,  ZHENG, Zhibing ,  LI, Song

IPC分类号： C07H15/18 ,  C07H15/10 ,  C07H15/04 ,  C07H1/00 ,  C07F7/10

摘要： Disclosed is a method for preparing a C-nucleoside compound represented by Formula (III) or salt thereof. The present method has a high reaction yield, is simple to operate, uses a single metal reagent, has stable reaction temperature conditions, does not require frequent changes to the reaction system during the operation process, is suitable for scale-up synthesis, is suitable for large-scale production of Remdesivir, and has low costs.

公开(公告)号：EP4190785A1

公开(公告)日：2023-06-07

申请号：EP21850321.7

申请日：2021-07-22

申请人： Sichuan University ,  Academy of Military Medical Sciences

发明人： QIN, Yong ,  ZHONG, Wu ,  XUE, Fei ,  ZHANG, Minjie ,  FAN, Shiyong ,  ZHENG, Zhibing ,  LI, Song

IPC分类号： C07D487/04

摘要： The present invention relates to the technical field of chemical drug synthesis, and specifically relates to a method for preparing a compound as shown in formula I, comprising: treating the compound as shown in formula VII with an acid to generate the compound as shown in formula I. The method has few synthetic process steps, raw materials which is stable and is easy to prepare, a reaction process which is easy to control, and a high overall yield and purity, and is suitable for industrial preparation.

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.