Synthesis of novel cyclic urea based HIV-1 protease inhibitors

A series of novel HIV-1 protease inhibitors was prepared in a short stereospecific manner. These compounds have only one P1 substituent interacting with the S1/S1' binding site of HIV-1 protease and only one hydroxyl group interacting with the catalytic aspartic acid domain, X-ray crystallography confirmed the desired R, R configuration of the final products.