New anti-retroviral desoxy:nojirimycin derivs.

摘要

Desoxynojirimycin derivs. of formula (I) and their salts are new. R1 = H or upto 10C alkyl, alkenyl or alkadienyl, all opt. substd. by halo, upto 8C alkoxy, 6-10 aryl or aryloxy or CONR6R7. R6, R7 = independently H, upto 8C acyl or alkyl, or phenyl (which may be substd. by upto 8C alkyl or alkoxy, halo or CF3 gp.). R2-R5 = independently H, COR8, 3-8C cycloalkyl (opt. substd. by upto 6C alkyl) or NR6R7, or R2 and R3, R3 and R4 or R4 and R5 together form -(CH2)n-, -C(R9)(R10)- or O(SiR11R12)2-. n = 1 or 2. R8 = upto 30C alkyl, alkenyl or alkadienyl or 6-10C aryl, which is opt. substd. by 1-2 independent halo, COOH or upto 8C alkyl, alkoxy or alkoxycarbonyl gps. R9-R12 = independently upto 8C alkyl or phenyl, which itself may be substd. by upto 8C alkyl. At least one of R2-R5 is not H. (I) may be prepd. e.g. from the correspg. N-substd. nojirimycin cpd. and a cpd. of formula Y-CO-Hal, O(COR8)2 or R13-N=C=O. Y has the same meanings as R2-R5 (but is not H); Hal - halogen, pref. Cl; and R13 = R6 or R7 (but not H). (I) is e.g. N-butenyl-4,6-isopropylidene-nojirimycin.