IE33493B1 - Substituted sulfanilamides - Google Patents

Abstract

1,247,993. Substituted sulphanilamides. F. HOFFMANN-LA ROCHE & CO. A.G. 22 July, 1969 [22 July, 1968], No. 36684/69. Heading C2C. Novel substituted sulphanilamides of the general formula wherein R and R<SP>1</SP> are C 1-18 alkylene groups, R<SP>2</SP> is a hydrogen atom or a C 1-7 alkyl group, m and n are 0 or 1, provided that at least one of m and n is 1, and A is a radical of one of the following formulµ wherein R<SP>4</SP> is a C 1-7 alkyl or C 1-7 alkoxy group or a halogen atom and p is 0, 1 or 2, and, where n is 0, salts thereof with pharmaceutically acceptable bases are prepared by acylation of a sulphanilamide of the general formula wherein B<SP>1</SP> is a hydrogen atom or a blocking group which can be hydrogenolysed or hydrolysed, or a salt thereof with one or more alkoxyalkanoic acids of the general formula and/or or reactive derivatives thereof and, when B<SP>1</SP> is a blocking group, removal of said blocking group by hydrogenolysis or hydrolysis, followed optionally by salification of the product. Substituted sulphanilamides of the general formula wherein r is 0 or 1 and B is a blocking group of the formula R<SP>3</SP>OCO- in which R<SP>3</SP> is a tertiary butyl group or a C 6-12 aryl-C 1-7 alkyl group, produced as intermediates in the above process when r is 1, are also novel. When r is 0, they are produced by acylation of the corresponding sulphanilamide of the fifth general formula above wherein B is a hydrogen atom. Pharmaceutical compositions having antibacterial activity comprise, as active ingredient, a substituted sulphanilamide of the first general formula above or, when n is 0, a salt thereof with a pharmaceutically acceptable base, in association with a compatible carrier and may be administered enterally or parenterally. [GB1247993A]