发明公开
EP0973755A1 ASYMMETRIC SYNTHESIS OF BENZOXAZINONES VIA NEW INTERMEDIATES
失效
不对称合成VEN BENZOXAZINOENÜBERNEUE ZWISCHENPRODUKTE
- 专利标题： ASYMMETRIC SYNTHESIS OF BENZOXAZINONES VIA NEW INTERMEDIATES
- 专利标题（中）： 不对称合成VEN BENZOXAZINOENÜBERNEUE ZWISCHENPRODUKTE
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申请号： EP98914408.4申请日： 1998-04-02
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公开(公告)号： EP0973755A1公开(公告)日： 2000-01-26
- 发明人: PIERCE, Michael, E. , CHEN, Cheng, Y. , CHOUDHURY, Anusuya , RADESCA, Lilian, A. , TAN, Lushi , ZHAO, Dalian
- 申请人： Du Pont Pharmaceuticals Company , Merck & Co., Inc.
- 申请人地址： 974 Centre Road, WR-1st 18 Wilmington, DE 19807 US
- 专利权人： Du Pont Pharmaceuticals Company,Merck & Co., Inc.
- 当前专利权人： Du Pont Pharmaceuticals Company,Merck & Co., Inc.
- 当前专利权人地址： 974 Centre Road, WR-1st 18 Wilmington, DE 19807 US
- 代理机构： Pett, Christopher Phineas
- 优先权： US42803P 19970407
- 国际公布： WO9845278 19981015
- 主分类号： C07D265/18
- IPC分类号： C07D265/18 ; C07C215/68 ; C07C211/52
摘要：
The present invention provides novel methods for the asymmetric synthesis of (S)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxazin-2-one of formula (VI-i) which is useful as a human immunodeficiency virus (HIV) reverse transcriptase inhibitor. In an embodiment, the present invention provides a process for the preparation of an amino alcohol compound of formula (V-i) comprising adding a toluene solution of 2,3-dichloro-5,6-dicyano-1,4-benzoquinone to a toluene solution of a compound of formula (III-i), via a compound of formula (IV-i).
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