| 摘要 |
PURPOSE:To obtain the title compound, an antibacterial, in high yield, by removing the protecting group from a cephalosporanic acid having an acyl group whose N- atom is protected with a specific acid in a specific solvent, and by acylating the reaction product with an active ester without isolating an intermediate. CONSTITUTION:A compound of formula I is reacted with an organic sulfonic acid in a nitrile solvent at 20-30 deg.C to remove the p-methoxybenzyloxycarbonyl group. The reaction product is then, without isolation of an intermediate, acylated with an active ester of formula II: (A is mono- or polycyclic nitrogen-containing six-membered aromatic heterocyclic ring) in the presence of an organic tertiary amine at 40 deg.C or below to give the desired compound of formula III. EFFECT:Combination of the nitrile solvent, organic sulfonic acid, and active ester permits a continuous process and a high purity of product. |
