QUINAZOLINE COMPOUNDS

摘要

Novel 2(1H)-quinazolinone derivatives having a group of the formual -A-Q-CO-R, wherein R is a lower alkyl, lower alkenyl, aralkyl, lower haloalkyl, lower alkoxyalkyl, lower hydroxyalkyl, lower mercaptoalkyl, cycloalkyl, lower cycloalkylalkyl group or a group of the formula R4 -N ANGLE R5 (wherein R4 and R5 are independently a hydrogen atom or a lower alkyl group, provided that R4 and R5 may form together with the adjacent nitorgen atom a 5- or 6- membered saturated heterocyclic ring, which may further contain a nitrogen or oxygen atom); Q is an oxygen or sulfur atom; and A is a lower alkylene group, at the 1-position of a quinazoline ring; are prepared by (a) reacting a 2(1H)-quinazolinone derivative having a hydrogen atom at the 1-position with a reactive ester of an alcohol of the formula R-CO-Q-A-OH, (b) reacting a 2-aminophenylketone derivative with cyanic acid or a salt thereof or a reactive ester of carbamic acid, (c) reacting a trihalogenoacetamideophenylketone derivative with ammonia, (d) reacting a 2-aminophenylketimine with a carbonic acid derivative, (e) reacting a 2(1H)-quinazolinone derivative having a A- QH group at the 1-position with a carboxylic acid of the formula R-COOH or a reactive derivative thereof, (f) reacting a reactive ester of a 2(1H)-quinazolinone derivative having a A-OH group at the 1-position with a carboxylic acid derivative of the formula R-CO-QH or a salt thereof, or (g) oxidizing a 3,4-dihydro-2(1H)-quinazolinone derivative having a group of the formula -A-Q-CO-R at the 1-position. These quinazolinone derivatives are useful as uricosuric, anti-inflammatory and/or analgesic agents.