To obtain a new compound having a stable non-peptidic structure to proteases existing in a large amount in organisms, and having specificity and excellent inhibiting activity to human acquired immune deficiency syndrome virus proteases.
This new compound is expressed by formula I [wherein, R1 is a (substituted) 8-16C aralkyloxycarbonyl, a (substituted) 7-15C arylcarbonyl or the like; R2 is a (substituted) 6-14C aryl; R3 is H, a (substituted) 1-10C alkyl or the like; R4 is a (substituted) 1-15C alkyl, a (substituted) 7-15C aralkyl or the like] and is e.g. N-{4-[acetyl-(1-tert-butylcarbamoyl-2-phenyl-ethyl)-amino]1- benzyl-2-hydroxy-butyl}-3-hydroxy-2-methylbenzamide. The compound of formula I is obtained e.g. by reacting a compound of formula II with an amino compound to obtain a compound of formula III, by reacting it with a metallized vinyl compound to obtain a compound of formula IV and then by the Michael addition reaction of it with an amine, followed by reducing the reaction product.
TAKAGI EIJI
OZAWA YUJI
SUGIYAMA AKIKO
