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1.发明公开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 有权工艺用于制备（1S，2R）-3 - [[（4-氨基苯基）磺酰基]（异丁基）氨基] -1-苄基-2-HYDROXYPROPYLCARBAMIDSÄURE-（3R，3AS，6AR）六氢呋喃并[2,3-B ]呋喃-3-基酯
公开(公告)号：EP1725566A1
公开(公告)日：2006-11-29
申请号：EP04805020.7
申请日：2004-12-23
发明人： GOYVAERTS, Nicolaas, Martha, Felix , WIGERINCK, Piet, Tom, Bert, Paul , ZINSER, Hartmut, Burghard , EBERT, Birgit, M.
IPC分类号： C07D493/04
CPC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.
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2.发明授权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 有权工艺用于制备（1S，2R）-3 - [[（4-氨基苯基）磺酰基]（异丁基）氨基] -1-苄基-2-HYDROXYPROPYLCARBAMIDSÄURE-（3R，3AS，6AR）六氢呋喃并[2,3-B ]呋喃-3-基酯
公开(公告)号：EP1725566B1
公开(公告)日：2009-06-17
申请号：EP04805020.7
申请日：2004-12-23
发明人： GOYVAERTS, Nicolaas, Martha, Felix , WIGERINCK, Piet, Tom, Bert, Paul , ZINSER, Hartmut, Burghard , EBERT, Birgit, M.
IPC分类号： C07D493/04
CPC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.
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