Process for the methyl-4-(dimethylamino)-3,5-dimethoxybenzoate
AssigneeHoffman-La Roche Inc.
InventorsAlfredo Guerrato, Martin Karpf, Hanny K. Berger, Ivan Kompis, Markus Schlageter
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Abstract
Methyl 4-dimethylamino-3,5-dimethoxybenzoate, an intermediate in the preparation of the antibacterially active aditoprim, is obtained from 4-amino-3,5-dibromobenzoic acid by replacement of the bromine atoms by methoxy groups and subsequent methylation.
Claims2
A process for the preparation of methyl 4-(dimethylamino)-3,5-dimethoxybenzoate which comprises reacting 4-amino-3,5-dibromobenzoic acid with an alkali methylate in the presence of Cu.sub.2 O and dimethylformamide or dimethylacetamide, and methylating the resulting 4-amino-3,5-dimethoxybenzoic acid with dimethyl sulfate in the presence of a base selected from the group consisting of lower aliphatic ketone and cycloaliphatic ketone, while heating, to yield methyl 4-(dimethylamino)-3,5-dimethoxybenzoate.
Dependencies are inferred from the claim text.