abstract |
1469448 Cephalosporin derivatives HOECHST AG 28 Nov 1974 [29 Nov 1973] 51644/74 Heading C2C Novel compounds I (in which R 1 , R 2 , and R 3 are H or alkyl, or R 1 and R 2 or R 2 and R 3 together may form an optionally substituted alkylene radical; X is a single bond or -NH-; A is phenylene or thienylene, which may be substituted; Y is a single bond or -O- and Z is a 5-6 membered ring system which may form part of a fused ring or be substituted) and salts and esters thereof are prepared by: (1) reaction of a compound II the carboxyl group of which may be protected or in the form of a salt, with an acid III or a reactive derivative thereof, and, if necessary, removing the protective group; (2) reaction of a compound IV with a thiol Z-SH; or (3) formation of a salt or ester from the free acid. The acid chlorides of the acids III may be prepared by reaction of the acid with SOCl 2 . Pharmaceutical compositions, useful as antibiotics, comprise a compound I, together with a suitable diluent and/or carrier and are administered orally or parenterally. |