PURPOSE: To provide new morpholin- and thiomorpholin-4-ylamide useful as inhibitors of human immunodeficiency virus-1-asparaginic acid protease in the treatment or prophylaxis of AIDS.
CONSTITUTION: The morpholin- and thiomorpholin-4-ylamide is compd. of formula I (R1 is H or lower alkyl; R2 is H, lower alkoxycarbonyl or the like; R3 is morpholino, thiomorpholino or the like; and R4 is H, OH or the like) or their salts, e.g., 5(S)-amino-6-cyclohexyl-4(S)-hydroxy-2(S)-isopropylhexanoyl-(L)- valyl-(L)-phenylalanyl-(thiomorpholin)-4-yl)amide. A compd. of the formula I (one of R1 and R2 is lower alkyl and the other is H or both R1 and R2 are lower alkyl) is obtd. by reacting an amino compd. of formula II with an alkylating reagent of the formula R-Y (R is lower alkyl corresponding to R1 and/or R2; and Y is a releasable group) in an aprotic polar solvent such as DMF preferably at -10 to +00°C.
AREKUSANDAA FUETSUSURAA
MARUKU RANKU
PEETAA SHIYUNAIDAA
