| abstract |
PURPOSE: To provide a new compd. which is useful as a protease inhibitor for retrovirus. n CONSTITUTION: This compd. is expressed by formula I. In formula I, Q is a single bond, NR 9 , NR 10 ; Z is O, NX; X is OH; Y is H, CH 2 OH or bonded with X to form epoxide; R 1 , R 2 are each H, an alkyl, a (CH 2 ) n -cycloalkyl ((n) is 0 to 4), a (CH 2 ) n -(substituted)-phenyl (wherein substituents are each a halogen, an alkoxide, an alkyl, phenyl); R 9 , R 10 are same as R 1 , R 2 but phenyl is not included in substituents; one of R 1 and R 2 may be bonded with one of R 9 and R 10 to form (H 2 ) m (wherein (m) is 3 or 4) or formula II; R 3 is an alkyl, a (CH 2 ) n alkyl, NHCOR 4 ; R 4 is UR 5 (wherein U is a single bond, O, NH; R 5 is an alkyl, a (CH 2 ) n -phenyl, etc.). The compd. (X and Y are bonded to form an epoxide) is obtd. by the reaction of a compd. expressed by formula III and m- chloroperbenzoate. The compd. expressed by formula III is obtd. from a compd. expressed by formula IV and a compd. expressed by formula V derived from 3-chloro-2-chloromethyl-1-propene as the starting material. n COPYRIGHT: (C)1992,JPO |