发明授权
US07772411B2 Process for the preparation of (3R,3aS,6aR)-hexahydrofuro [2,3-b] furan-3-yl (1S,2R)-3[[(4-aminophenyl) sulfonyl] (isobutyl) amino]-1-benzyl-2-hydroxypropylcarbamate
有权
制备(3R,3aS,6aR) - 六氢呋喃并[2,3-b]呋喃-3-基(1S,2R)-3 [[(4-氨基苯基)磺酰基](异丁基)氨基] -1- 苄基-2-羟丙基氨基甲酸酯
- 专利标题: Process for the preparation of (3R,3aS,6aR)-hexahydrofuro [2,3-b] furan-3-yl (1S,2R)-3[[(4-aminophenyl) sulfonyl] (isobutyl) amino]-1-benzyl-2-hydroxypropylcarbamate
- 专利标题(中): 制备(3R,3aS,6aR) - 六氢呋喃并[2,3-b]呋喃-3-基(1S,2R)-3 [[(4-氨基苯基)磺酰基](异丁基)氨基] -1- 苄基-2-羟丙基氨基甲酸酯
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申请号: US10596732申请日: 2004-12-23
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公开(公告)号: US07772411B2公开(公告)日: 2010-08-10
- 发明人: Nicolaas Martha Felix Goyvaerts , Piet Tom Bert Paul Wigerinck , Hartmut Burghard Zinser , Birgit M. Ebert
- 申请人: Nicolaas Martha Felix Goyvaerts , Piet Tom Bert Paul Wigerinck , Hartmut Burghard Zinser , Birgit M. Ebert
- 申请人地址: IE
- 专利权人: Tibotec Pharmaceuticals Ltd.
- 当前专利权人: Tibotec Pharmaceuticals Ltd.
- 当前专利权人地址: IE
- 优先权: EP03104949 20031223
- 国际申请: PCT/EP2004/053692 WO 20041223
- 国际公布: WO2005/063770 WO 20050714
- 主分类号: C07D493/04
- IPC分类号: C07D493/04
摘要:
The present invention relates to a process for the preparation of (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl (1S,2R)-3-[[(4-aminophenyl)sulfonyl](isobutyl) amino]-1-benzyl-2-hydroxypropylcarbamate as well as intermediates for use in said process. More in particular the invention relates to processes for the preparation of (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl (1S,2R)-3-[[(4-aminophenyl)sulfonyl](isobutyl)amino]-1-benzyl-2-hydroxypropylcarbamate which make use of 4-amino-N-((2R,3S)-3-amino-2-hydroxy-4-phenylbutyl)-N-(isobutyl)benzene sulfonamide intermediate, and to processes amenable to industrial scaling up. (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl (1S,2R)-3-[[(4-aminophenyl)sulfonyl](isobutyl)amino]-1-benzyl-2-hydroxypropylcarbamate is particularly useful as HIV protease inhibitors.