摘要 |
<p>Cephalosporin derivs. of formula (I) (where X is H, HOOC-CH(NHZ)-(CH2)3-CO-, or D-(-) Z is H or a protecting gp. -OCOR, -CONHR or -COR; R is 1-20C (halo)alkyl or aryl, pref. n is 0-6; R2 and R3 are each H, Cl, Br, F, NO2, lower alkyl or alkoxy are prepd. by (a) treating a cpd. of formula (II) (where M is H or a cation; Y is (III) with a 5-mercapto-1,2,3-triazole of formula (IV) or its salt, to produce a cpd. of formula (V), (b) cleaving the 7-amido gp. on (V) to give 7-amino-3-(5-(1,2,3-triazol-5-yl)thiomethyl)-3-cephem-4-carboxyli- c acid (VI) and (c) opt. acylating (VI) with a deriv. of D-(-) acid (VII) (where B is protecting gp) and eliminating the protecting gp. B. (I) are antibiotics and inters. for antibiotics, active against both Gram positive and negative bacteria.</p> |