| 摘要 |
<p>Derivatives of cephalosporin C are produced by reacting in a polar medium a compound of the general formula <FORM:1012943/C2/1> (in which R1 is an acyl group and R2 and R3/h are each hydrogen atoms or R2 is a hydrogen atom and R3 is an acyl group or a triaryl substituted alkyl group, or R2 and R3 together form a divalent acyl group) or a salt thereof, with a strong nucleophile selected from (a) thiourea and substituted thioureas, (b) aromatic and aliphatic thioamides, (c) thiophenol and substituted thiophenols, (d) substituted and unsubstituted primary and secondary aromatic amines, (e) thiols and substituted thiols, (f) metal azides, metal hydrogen phosphates and metal thiosulphates, and (g) pyrroles and substituted pyrroles. The Specification contains lists of suitable reactants of the above types and describes the production of many derivatives. Pharmaceutical compositions comprise the above derivatives formulated for administration in any convenient way such as injectable preparations in solution or suspension in a suitable medium; mixed with solid excipients they may be compressed into tablets or filled into capsules, and they may also be mixed with suitable bases for presentation as suppositories.</p> |
