QUARTERNARY AMMONIUM SALT DERIVATIVE AND ITS APPLICATION

摘要

PROBLEM TO BE SOLVED: To obtain a prodrug having decreased toxicity, excellent solubility and strong CCR5 antagonism and useful as a preventive/therapeutic agent for infectious diseases of HIV or the like. SOLUTION: This prodrug is represented by formula I [R1 is (substituted) phenyl or (substituted) thienyl; Y is CH2, O or S; R2 to R4 are each a (substituted) aliphatic hydrocarbon or (substituted) alicyclic heterocycle] and preferably N,N'-dimethyl-N-(4-(((2-(4-methylphenyl)-6,7-dihydro-5H- benzocycloheptenyl) carbonyl)amino)benzyl)-N-(4-tetrahydropyranyl)ammonium chloride or the like. The above-mentioned compound is obtained by condensing a compound of formula II with a aniline derivative of formula III (X is a halogen or the like), in a solvent such as N,N-dimethylformamide, at about -20 to 50 deg.C and for about 1 to about 100 h.