2 displacement methyl 2,3 dihydroimidazo (1,2c) quinazoline 5 (6H) - on (- thione), the production manner and its application

摘要

PURPOSE: To obtain a new 2-substd. methyl2,3-dihydroimidazo[1,2c]quinazolin5(6 H)-one (-thione) having α₁-adrenalin receptor antagonism activity and useful in the prevention and treatment of hypertension, etc. ;CONSTITUTION: The 2-substd. methyl-2,3-dihydroimidazo[1,2-c]quinazolin-5(6H)- one (-thione) is a compd. of formula I [where X is O or S; R₁ and R₂ are each H, a lower alkyl, an aryl, etc.; R₁ and R₂ may bond to each other to form a 4-10C alkylene, etc.; and R₃ and R₄ are each a halogen, H, an alkyl, trifluoromethyl, etc.], e.g. 2-(4-phenyl1-piperazinyl)methyl2,3dihydroimidazo[1,2 c]quinazolin-5(6H)-one. The compd. of formula I is obtd. by allowing a compd. of formula III (where Y is a halogen) obtd. by using a compd. of formula II as starting material to react with a compd. of IV in a solvent such as THF in the presence of a base such as triethylamine.;COPYRIGHT: (C)1993,JPO