发明授权
US09061991B2 Method for producing 1-amino-1-alkoxycarbonyl-2-vinylcyclopropane
有权
1-氨基-1-烷氧基羰基-2-乙烯基环丙烷的制备方法
- 专利标题： Method for producing 1-amino-1-alkoxycarbonyl-2-vinylcyclopropane
- 专利标题（中）： 1-氨基-1-烷氧基羰基-2-乙烯基环丙烷的制备方法
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申请号： US13579045申请日： 2011-02-16
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公开(公告)号： US09061991B2公开(公告)日： 2015-06-23
- 发明人: Yuuki Asuma , Tatsuya Suzuki , Jun Takehara , Tsugihiko Hidaka , Kuniko Asada , Ryoma Miyake , Yasumasa Dekishima , Hiroshi Kawabata
- 申请人： Yuuki Asuma , Tatsuya Suzuki , Jun Takehara , Tsugihiko Hidaka , Kuniko Asada , Ryoma Miyake , Yasumasa Dekishima , Hiroshi Kawabata
- 申请人地址： JP Tokyo
- 专利权人： API CORPORATION
- 当前专利权人： API CORPORATION
- 当前专利权人地址： JP Tokyo
- 代理机构： Greenblum & Bernstein, P.L.C.
- 优先权： JP2010-031322 20100216
- 国际申请： PCT/JP2011/053285 WO 20110216
- 国际公布： WO2011/102388 WO 20110825
- 主分类号： C07C1/32
- IPC分类号： C07C1/32 ; C07C13/04 ; C07C67/343 ; C07B53/00 ; C07B57/00 ; C07C67/313 ; C07C227/04 ; C07C227/32 ; C07C269/02 ; C07C247/22 ; C12P41/00 ; C12P7/62
摘要：
It is an object of the present invention to provide a novel method for producing (1R,2S)/(1S,2R)-1-amino-1-alkoxycarbonyl-2-vinylcyclopropane which is useful as a synthetic intermediate of therapeutic agents for hepatitis C and a synthetic intermediate thereof. According to the present invention, when a trans-2-butene derivative having a leaving group at each of the 1- and 4-positions is reacted with a malonic ester in the presence of a base, a specific amount of an alkali metal alkoxide or an alkali metal hydride is used as the base, and further a specific amount of a malonic ester is used to produce a cyclopropane diester, and further, chiral or achiral 1-amino-1-alkoxy-carbonyl-2-vinylcyclopropane and a salt thereof are synthesized using the cyclopropane diester.