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公开(公告)号:EP3359522B1
公开(公告)日:2020-02-26
申请号:EP16853064.0
申请日:2016-09-09
发明人: WU, Shengwen , LI, Wenge , WU, Lei , ZOU, Li , HU, Siming , XU, Tengyue , LIU, Hongfeng , TAO, Yi , CHI, Yongxiang
IPC分类号: C07C271/16 , C07C269/06 , C07C271/18 , C07C269/00 , C07C231/12 , C07C233/47 , C07C271/22 , C07C233/18 , C07C271/64
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公开(公告)号:EP3359522A1
公开(公告)日:2018-08-15
申请号:EP16853064.0
申请日:2016-09-09
发明人: WU, Shengwen , LI, Wenge , WU, Lei , ZOU, Li , HU, Siming , XU, Tengyue , LIU, Hongfeng , TAO, Yi , CHI, Yongxiang
IPC分类号: C07C271/16 , C07C269/06 , C07C271/18 , C07C269/00
CPC分类号: C07C269/06 , C07C231/12 , C07C269/00 , C07C271/64 , C07C233/47 , C07C271/22 , C07C233/18
摘要: A process is provided for preparation of (R)-N-Boc biphenyl alaninol.It provides a preparation process for a compound outlined as compound 4, which includes these operations: in one of the alcohol solvents, asymmetric hydrogenation of 5 in the presence of [Rh(Duanphos)(X)]Y and hydrogen to provide compound 4. Here "Duanphos" is (Rc,Sp)-Duanphos or (Sc,Rp)-Duanphos; X is NBD or/and COD; Y is one or more of BF4, PF6, SbF6. This process has a lot of advantages, such as low cost, safe operation, less pollution and high yield. The product was obtained in >99% purity and ee which is suitable to scale up in industrial scale.
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公开(公告)号:EP4029853A1
公开(公告)日:2022-07-20
申请号:EP20863253.9
申请日:2020-09-10
发明人: WU, Shengwen , LI, Wenge , ZHOU, Peng
IPC分类号: C07D213/89 , C07C209/58 , C07C213/06 , C07D213/127 , C07D213/12 , C07D213/04 , C07C255/07 , A61P35/00 , A61K31/33
摘要: The present application provides a compound of formula II and a method for preparing a compound of formula I, i.e., 2-iso-propyl-4-methylpyridin-3-amine by using the same. The compound of formula I can be applied to synthesis of KRAS inhibitor drugs. The raw materials involved in the method of the present application are easy to obtain and low in price, operation is easy and convenient, economization and environmental protection are achieved, and industrial production is facilitated.
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