METHOD OF PRODUCING 1-ALKYL-4-PHENYL-2/1H/QUINAZOLINES EVENTUALLY 1-ALKYL-4-/2'-THIENYL/-2/1H/QUINAZOLINES

摘要

1383255 4-Aryl-quinazolinones SANDOZ Ltd 4 July 1972 [8 July 1971] 31161/72 Heading C2C Novel compounds of Formula I (R 1 is 1-5C alkyl; R 2 and R 3 are H, or 1-3C alkyl and R 4 is a radical of Formula IX or X in which Y and Y 1 are H, F, Cl, 1-2C alkyl, 1-2C alkoxy, or CF 3 , provided if one is CF 3 , the other must be H; and Y 2 is H, F, Cl or 1-3C alkyl), are prepared by cyclizing a compound of Formula II or an alkali or alkaline earth metal salt thereof with phosgene, a 1-2C alkyl ehlorocarbonate or 1,1SP1/SP-carbonyl-di-imidazole. Compounds of Formula I may be dehydrogenated to give compounds of Formulae VII and VIII Compounds of Formula II may be prepared by reaction of a compound of Formula III with a strong alkali or alkaline earth metal base and a compound of formula R 4 CN. Compounds of Formula III may be prepared by reaction of a compound of Formula V with a compound of formula R 1 NH 2 . Pharmaceutical compositions for administration as anti-inflammatory agents and as analgesics comprise a compound of Formula I together with a suitable carrier or diluent.