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    Method for Preparing Key Intermediate of ABT-737 and Method for Preparing ABT-737
    5.
    发明公开
    Method for Preparing Key Intermediate of ABT-737 and Method for Preparing ABT-737 审中-公开

    公开(公告)号：US20240140923A1

    公开(公告)日：2024-05-02

    申请号：US17597868

    申请日：2021-06-17

    申请人： Xeon Biopharmaceutical Limited

    发明人： Yanfei GU ,  Yao HE

    IPC分类号： C07D295/155 ,  C07C227/18 ,  C07C303/40 ,  C07C319/14 ,  C07C319/20

    CPC分类号： C07D295/155 ,  C07C227/18 ,  C07C303/40 ,  C07C319/14 ,  C07C319/20

    摘要： The present disclosure relates to the technical field of drug synthesis, and provides a method for preparing a key intermediate of ABT-737 and a method for preparing ABT-737. In the present disclosure, the compound having a structure represented by formula I is used as the starting material. The carboxyl group in the compound having a structure represented by formula I is first reduced to a hydroxyl group, followed by a vulcanization by a vulcanizing agent, and then an amination, a deprotection, a condensation, and a carbonyl group reduction, to obtain the key intermediate of ABT-737 having a structure represented by formula VI. Tert-butoxycarbonyl is used as the protecting group for the compound having a structure represented by formula I, and the subsequent intermediate containing the protecting group of tert-butoxycarbonyl is stable, and easy to be deprotected. This method is suitable for mass synthesis, with high product yield and low production cost, and thus has a good industrialization prospect.

    Green cationization agent
    7.
    发明授权
    Green cationization agent 有权

    公开(公告)号：US11884753B2

    公开(公告)日：2024-01-30

    申请号：US17825473

    申请日：2022-05-26

    申请人： SACHEM, INC.

    发明人： Tim Engel

    IPC分类号： C08B37/00 ,  C07C227/18 ,  C07C229/12 ,  C07D303/16

    CPC分类号： C08B37/0096 ,  C07C227/18 ,  C07C229/12 ,  C07D303/16

    摘要： A compound having Formula (I) or Formula (II):






    or a mixture thereof,
    in which R is —H; —CH3; —CH—(CH3)2; —CH2—CH—(CH3)2; —CH—(CH3)—CH2—CH3; —CH2—(C6H5); —CH2—(3-indole); —CH2—CH2—S—CH3; —CH2—OH; —CH—(CH3)—OH; —CH2—SH; —CH2-(p-C6H4OH); —CH2—CH2—CH2—CH2—NH2; —CH2—CO—NH2; —CH2—CH2—CO—NH2; —CH2—CH2—COOH; —CH2—COOH; or —CH2—CH2—NH—C═NH2(NH2);
    and X is a suitable non-interfering anion, a process for making the compound having Formula (I) or Formula (II), and a process for reacting the compound having Formula (I) or Formula (II) or a mixture thereof with a (poly)saccharide to form a cationized (poly)saccharide.