Process for Preparation of (1S, 2R) - 3 - (4-aminophenyl) (Isobutyl) sulfonyl) amino) - 1 - Benzyl - 2 - hidroxipropilcarbamato (3R, 3aS, 6aR) - hexahidrofuro - (2,3-b) furan-3 - ilo (darunavir) and Intermediate compounds useful in the process.

摘要

Claim 1, a process for the preparation of darunavir of formula (1) or a Salt or solvate, addition or pseudopolimorfica polymorphic form of (i), which comprises reacting a compound of formula (2) where pg represents an amino Protecting Group, with N - Benzyl - isobutilamina,That is a compound of formula (3) to produce a compound of formula (4); (ii) discuss the compound of formula (4) to delete the Group pg Protector for a compound of formula (5); (iii) coupling Compound of the formula (5) with a Derivative of (3R, 3aS, 6aR) - hexahidrofuro [23 - B] furan - 3 - ILO to obtain a compound of formula (6); (iv) to eliminate the n-benzyl Group of the compound of formula (6) to produce a compound of formula (7); (V) introduce a nitrofenilsulfonilo P - Group in the compound of formula (7) to obtain a compound of formula (8); (VI) reduce the gr Upo Nitro Compound of formula (8) to darunavir or solvate form,Salt Addition or pseudopolimorfica polymorphic form or the same.