公开(公告)号：EP0973755A1

公开(公告)日：2000-01-26

申请号：EP98914408.4

申请日：1998-04-02

申请人： Du Pont Pharmaceuticals Company ,  Merck & Co., Inc.

发明人： PIERCE, Michael, E. ,  CHEN, Cheng, Y. ,  CHOUDHURY, Anusuya ,  RADESCA, Lilian, A. ,  TAN, Lushi ,  ZHAO, Dalian

IPC分类号： C07D265/18 ,  C07C215/68 ,  C07C211/52

CPC分类号： C07D265/18 ,  C07C213/00 ,  C07C213/02 ,  C07C221/00 ,  C07C2601/02 ,  C07C215/68 ,  C07C217/58 ,  C07C225/22

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).

摘要翻译： 本发明提供了用于不对称合成式（Ⅵ-ⅰ）的（S）-6-氯-4-环丙基乙炔基-4-三氟甲基-1,4-二氢-2H-3,1-苯并恶嗪-2-酮的新方法 ），其可用作人类免疫缺陷病毒（HIV）逆转录酶抑制剂。