GB985692A - New sulphanilamide derivatives and processes for their production - Google Patents

Abstract

The invention comprises sulpha-pyrimidine compounds of the formula <FORM:0985692/C2/1> wherein R1 is chlorine or a C1- 5 alkoxy radical and R2 is a C1- 5 alkyl radical, and their preparation either by (a) reacting a salt of a benzenesulphonamide p-substituted by an amino group or a nitrogen-containing group convertible to an amino group, with an appropriate pyrimidine compound bearing a chlorine, C1- 5 alkylthio, C1- 5 alkylsulphonyl or trimethylammonium substituent in the 2-position or (b) reacting a functional derivative of a benzenesulphonic acid such as the sulphonyl chloride, p-substituted by a nitrogen-containing group convertible to an amino group with an appropriate 2-amino-pyrimidine; and in both processes (a) and (b), if appropriate and in any desired order, converting the p-substituent to an amino group by hydrolysis or reduction and replacing a chlorine atom R1 by an alkoxy radical. Suitably, the p-substituted convertible to an amino group may be an acylamino, e.g. acetylamino or carbalkoxyamino, benzylideneamino, p-dimethylaminobenzylideneamino, nitro, phenylazo or p-dimethylaminophenylazo radical. N - (4,6 - Dimethoxy - 5 - chloro - 2 - pyrimidyl)- N,N,N - trimethylammonium chloride and N - (4,5 - dichloro - 6 - methoxy - 2 - pyrimidyl) - N,N,N - trimethylammonium chloride are made by the action of trimethylamine on the corresponding 2-chloro-pyrimidine compound. Pharmaceutical preparations comprises the above sulphanilamido-pyrimidines or their salts with pharmaceutically acceptable bases such as alkali metals, magnesium, calcium, ethylamine, diethylamine, dimethylamine, morpholine, ethylenediamine, aminoethanol, diethylaminoethanol and di- or tri-ethanolamine. The preparations may take forms suitable for internal or external use such as tablets, dragees, suppositories, syrups, powders, capsules or aqueous solutions for injection.