PRODUCTION OF BENZO(C)PHENANTHRIDINUM DERIVATIVE AND ITS NEW COMPOUND

摘要

PURPOSE:To obtain the subject compound useful as a medicine having antitumor activity and inhibitory action on blood platelet aggregation by converting a naphthylamine derivative into benzo[c]phenanthridine and then N-alkylating. CONSTITUTION:A compound of formula I (M and N are OH, lower alkoxy or M and N are both H or bonded to form methylenedioxy; Y is halogen; Y is protecting group) is subjected to ring closure reaction with an organotin hydride (e.g. tri-n-butyltin hydride) and further aromatized by oxidation to give a compound of formula II. Then the compound of formula II is N-alkylated with an N-alkylating agent (e.g. methyl-p-toluenesulfonate), deprotected and treated with an acid to give the objective compound of formula III. 2,3-(Methylenedioxy)-5-methyl-7-hydroxy-8-methoxy- benzo[c]phenanthridinium.hydride may be cited as the compound of formula III.