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
    1.
    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
    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

    公开(公告)号:US07772411B2

    公开(公告)日:2010-08-10

    申请号:US10596732

    申请日:2004-12-23

    IPC分类号: C07D493/04

    CPC分类号: C07D493/02 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.

    摘要翻译: 本发明涉及制备(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-羟基丙基氨基甲酸酯以及用于所述方法的中间体。 更具体地,本发明涉及制备(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] 使用4-氨基-N - ((2R,3S)-3-氨基-2-羟基-4-苯基丁基)-N-(异丁基)苯磺酰胺的(异丁基)氨基] -1-苄基-2-羟基丙基氨基甲酸叔丁酯 中间和适用于工业规模化的流程。 (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- 羟丙基氨基甲酸酯特别可用作HIV蛋白酶抑制剂。