Simplified procedure for preparation of darunavir

The present invention relates to an improved process for preparing [(1S,2R)-3-[[(4-aminophenyl)-sulfonyl](2-methylpropyl)amino]-2-hydroxy-1-(phenylmethyl)-propyl]-carbamic acid (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl ester, which compound is also known under its INN as darunavir, by reacting carbonic acid 2,5-dioxo-1-pyrrolidinyl [(3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl]ester with 4-amino-N-[(2R,3S)-3-amino-2-hydroxy-4-phenylbutyl]-N-(2-methylpropyl)-benzenesulfonamide in ethanol as solvent. Furthermore the process allows for darunavir to be isolated immediately in its ethanolate form, i.e. darunavir monoethanolate, which is the marketed form of darunavir under the tradename PrezistaTM. 本发明涉及一种用于制备[(1S,2R)-3-[[(4-氨基苯基)-磺酰基](2-甲基丙基)氨基]-2-羟基-1-(苯基甲基)-丙基]-氨基甲酸(3R,3aS,6aR)-六氢呋喃并[2,3-b]呋喃-3-基酯的改进的方法-该化合物还以其作为达芦那韦的INN已知-该方法通过使碳酸2,5-二氧-1-吡咯烷基[(3R,3aS,6aR)-六氢呋喃并[2,3-b]呋喃-3-基]酯与4-氨基-N-[(2R,3S)-3-氨基-2-羟基-4-苯基丁基]-N-(2-甲基丙基)-苯磺酰胺在作为溶剂的乙醇中反应。此外，所述方法允许达芦那韦以其乙醇化物形式(即达芦那韦单乙醇化物)直接分离，该形式是达芦那韦以商品名Prezista的销售形式。