A method for the preparation of phthalic azins

摘要

Novel compounds of formula FORM:1094044/C2/1 wherein R is H, C1-C6 alkyl, C1-C6 alkoxy, di - (C1-C6) - alkyl amino - (C1-C6) - alkoxy, phenyl, phenyl - (C1-C6) - alkyl, pyridyl - (C1-C6) - alkyl, carbo - (C1-C6 - alkoxy - (C1-C6) - alkyl, carboxy - (C1-C6) - alkyl, carbo - hydrazino - (C1-C6) - alkyl, anilino or carbamyl-(C1-C6)-alkyl, R1 is H, C1-C6 alkyl, phenyl or phenyl-(C1-C6) alkyl, R2 is H, C1-C6 alkyl or alkanoyl and where the benzenoid portion of the phthalazine nucleus and/or the phenyl group(s) of R or R1 when present may optionally be substituted by one or more halogen atoms or C1-C6 alkyl, C1-C6 alkoxy, NO2, NH2, di - (C1-C6) alkyl amino or carboxy groups, and acid addition and quaternary ammonium salts thereof, are prepared mainly by reaction of a compound of formula FORM:1094044/C2/2 with a compound R1-NH-OR2, or, in the case where R is carboxyalkyl, by hydrolysis of a compound where R is carboalkoxyalkyl, or, where R is carbohydrazinoalkyl, by reaction of hydrazine hydrate with a compound where R is carboalkoxyalkyl, or, in the case where R2 is alkanoyl, by reaction of an alkanoic acid anhydride with a compound where R2 is H. Pharmaceutical compositions in conventional forms comprise an above novel compound or an acid addition or quaternary ammonium salt thereof and a carrier therefor.