| 摘要 |
Syn 7-[2-(2-protected-amino-4- thiazolyl)-2-substituted-imino- acetamido]-ceph-3-em-4-carboxylic acid derivatives, which have pharmacological activity or may be used in the preparation of pharmacologically-active compounds, are prepared by reacting a syn 2-(2- protected-amino-4-thiazolyl)-2- substituted-imino-acetic acid or salt thereof with a compound of the general formula: <IMAGE> (wherein Y represents a tosyl or mesyl ion and Z represents a halogen ion, Y and Z each represent a tosyl ion, or Y and Z each represent a mesyl ion) and optionally treating the product with a base, so as to obtain the corresponding syn 2-(2-protected- amino-4-thiazolyl)-2-substituted- iminoacetoxy-tris(dimethylamino)- phosphonium salts, which salt is thereafter treated, optionally in the presence of a base, with an optionally 3/4 substituted 7-amino- cephalosporanic acid, or S-oxo or S,S- dioxo derivative, or a salt or ester thereof, and then treated with an acid. The acylation of the phosphonium salt is preferably carried out in an organic solvent below 0 DEG C, or in an aqueous solvent at ambient temperature. |
