| abstract |
PURPOSE: To provide novel anhydrostachine phosphonopyrrolidines and piperidines which have extremely strong actions on retroviruses and are useful as human antivirus agents and veterinary drugs. n CONSTITUTION: This compd. is expressed by formula I [W is H, typical amino protective group, (substd. by 6 to 10C aryl) alkyl or alkenyl, R 3 -CO-, R 5 R 4 N-CO-, R 6 -SO 2 - (R 3 is H, CF 3 , alkoxy, alkyl, aryl, etc.; R 4 , R 5 are H, aryl, etc., R 6 is alkyl); A, B, D are direct bonds; formula II, formula III (x, x' are 1, 2), etc.; R 1 is cycloalkyl, alkyl, etc.; R 2 is -CO-NR 4 R 5 , etc.] and the physiologically permissible salt thereof; for example, the compd. of formula IV. The compd. of the formula I is obtd. by bringing, for example, the compd. of formula V and the compd. of formula IV into reaction with each other. n COPYRIGHT: (C)1992,JPO |