- 专利标题： METHOD FOR SYNTHESIZING NOVEL CHIRAL LIGAND, METAL CHELATE, A VARIETY OF NON-NATURAL AMINO ACIDS, MARAVIROC AND KEY INTERMEDIATE THEREOF
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申请号： EP17854729.5申请日： 2017-09-19
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公开(公告)号： EP3521274A1公开(公告)日： 2019-08-07
- 发明人: LIU, Hong , WANG, Jiang , ZHOU, Shengbin , PENG, Panfeng , NIAN, Yong , WANG, Shuni , SHU, Shuangjie , SHEN, Hao , JIANG, Hualiang , CHEN, Kaixian
- 申请人： Shanghai Institute of Materia Medica, Chinese Academy of Sciences
- 申请人地址： 555 Zu Chong Zhi Road Zhang Jiang Pudong Shanghai 201203 CN
- 专利权人： Shanghai Institute of Materia Medica, Chinese Academy of Sciences
- 当前专利权人： Shanghai Institute of Materia Medica, Chinese Academy of Sciences
- 当前专利权人地址： 555 Zu Chong Zhi Road Zhang Jiang Pudong Shanghai 201203 CN
- 代理机构： Lavoix
- 优先权： CN201610871043 20160929
- 国际公布： WO2018059279 20180405
- 主分类号： C07D207/16
- IPC分类号： C07D207/16 ; C07D409/12 ; C07F15/04 ; C07C227/34 ; C07C229/34 ; C07D401/04
摘要：
Disclosed is a method for synthesizing a novel chiral ligand, a metal chelate, a variety of non-natural amino acids, Maraviroc and a key intermediate thereof. In the invention, (R)-2-methyl proline is selected and used as a starting raw material, (S)-β 3 -amino acid is obtained by asymmetric resolution induced by using a nickel chelate, and Maraviroc is synthesized by using (S)-3-amino-3-phenylpropionic acid as a key intermediate with a high yield and the ee value reaching 98.2% or more. The method of the present invention has widely available materials, mild synthetic process conditions, is easy to control, and produces a product of a high optical purity.
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