| abstract |
The present invention relates to a process for the preparation of hydroxyethylamine compounds which are effective as retroviral protease inhibitors, and in particular as HIV protease inhibitors. These compounds have the formula: <IMAGE> or a pharmaceutically acceptable salt, pro-drug or ester thereof, in which A represents, for example, a radical of the formula: <IMAGE> in which R represents, for example, hydrogen or alkoxycarbonyl; R' represents, for example, hydrogen or is as defined for R3; t represents 0 or 1; R1 represents, for example, -CH2SO2NH2 or hydrogen; R1' and R1" represent hydrogen or are as defined for R1; R2 represents, for example, alkyl or aryl; R3 represents, for example, alkyl or alkenyl; Y and Y' represent O or S; R4 and R5 represent, for example, hydrogen or are as defined for R3; R6 represents hydrogen or is as defined for R3; and R20 and R21 are as defined for R1. Said process consists, for example, in the reaction of a compound of formula: <IMAGE> after removal of the amino protecting group P and neutralization of the amine salt obtained with a compound of the formula: <IMAGE> |