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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: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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