IMIDAZO-AND PYRIMIDO (2,1-B) QUINAZOLINES PREPARATION THEREOF

摘要

Imidazo- and pyrimido2,1-b!quinazolines of the formula, wherein R1 and R2 are independently hydrogen or halogen or phenyl; R3 is hydrogen or phenyl R4 is hydrogen, C1-4 alkyl or phenyl; and A is C2-3 alkylene which may be substituted by one or two C1-2 alkyl radicals, and pharmaceutically acceptable acid addition salts thereof, are prepared by (a) reacting a compound of the formula, wherein R1, R2, R3, R4 and A are as defined above; and X is oxygen or sulfur, with a halogenating agent at a temperature of about 30.degree.C to about 180.degree.C or (b) reacting a compound of the formula (V) wherein R1, R2, and A are as defined above; R'3 is phenyl, Y1 is halogen or arylsulfonyl selected from the group consisting of benzenesulfonyl and p-toluenesulfonyl; and Y2 is halogen or C1-4 alkylthio, with a compound of the formula R4 - NH2 wherein R4 is as defined above, at a temperature from room temperature to 160.degree.C. In the above imidazo- and pyrimido 2,1-b! quinazolines, those having phenyl as R3 are novel compounds and show antidepressant and/or antihypertensive activities.