SUBSTITUIERTE ACETAMIDOCEPHALOSPORINE, IHRE SALZE MIT BASEN, VERFAHREN ZU IHRER HERSTELLUNG UND ARZNEIMITTEL

1449398 Cephalosporin derivatives SMITHKLINE CORP 20 Dec 1974 [26 Dec 1973] 55124/74 Heading C2C Novel compounds I (n is 0, 1 or 2; X is H, -OCOCH 3 , -OCH 3 , -SCH 3 , or -SHet; and Het is a 5 or 6- membered heterocyclic ring containing C and 1-4 atoms selected from N, O and S, optionally substituted by one or two substituents selected from 1-6C alkyl or alkoxy, allyl, allyloxy, methoxymethyl, halo, cyclopropyl, carbamyl, -COOH, 2-7C alkoxycarbonyl, SH, -SCH 3 , CF 3 , OH, NH 2 , 1-6C alkylamino and di(1-6C alkyl)amino; and where Het contains a N atom, the N oxides thereof) and salts thereof are prepared by acylation of the appropriate 7-aminoceph-3-em-4-carboxylic acid. Intermediates isolated are trifluoroethylmercaptoacetyl chloride, prepared from the acid and SOCl 2 ; N - hydrozysuccinimidyl trifluoroethylsulphinylacetate, prepared by esterification of CF 3 CH 2 SCH 2 COOH with N-hydroxysuccinimide followed by reaction with m-chloroperbenzoic acid; and trifluoroethylsulphonylacetic acid, prepared by oxidation of the methyl ester of trifluoroethylmercaptoacetic acid. Antibacterial compositions comprise a compound I together with a suitable pharmaceutical excipient.