Process for the preparation of (1S, 2R) -3 - [[(4-aminophenyl) sulfonyl] (isobutyl) amino] -1-benzyl-2-hidroxipopilcarbamato of (3R, 3aS, 6aR) -Hexahydrofuro [2,3- b] furan-3-yl
2009
A process for the preparation of darunavir of formula (A), or a solvate, addition salt or polymorphic or pseudopolymorphic form thereof: Formula ** ** comprising: (i) reacting a compound of formula (1): ** ** formula wherein PG represents an amino protecting group, with N-benzyl-isobutylamine, namely a compound of formula (2): ** ** formula to obtain a compound of formula (3): * * ** formula (ii) treating the compound of formula (3) to remove the protecting group PG to obtain a compound of formula (4): ** ** formula (iii) coupling the compound of formula (4) with a derivative of (3R, 3aS, 6aR) -Hexahydrofuro [2,3-b] furan-3-yl, to give a compound of formula (5): ** ** formula (iv) removing the N-benzyl group of compound of formula (5), to obtain a compound of formula (6): ** ** formula (v) introducing a p-nitrophenylsulfonyl group in the compound of formula (6) to obtain a compound of formula (7): ** ** formula (vi) reducing the grup or nitro compound of formula (7) to form darunavir or a solvate, addition salt or polymorphic or pseudopolymorphic form thereof.
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