NOVEL PROCESS FOR MANUFACTURING CEPHALOSPORIN DERIVATIVES

摘要

PURPOSE: Provided is a novel process for the manufacture of cephalosporin derivatives to offer easier access to pharmacologically useful cephalosporins. CONSTITUTION: Cephalosporin derivatives are represented by the formula(I), wherein R1 is an amino protecting group, R2 is a carboxy protecting group and R is hydrogen, lower alkyl, lower alkoxy, cycloalkyl, cycloalkenyl, cycloalkyl-lower alkyl, lower alkenyl, lower alkynyl, aryl, aryl-lower alkyl, heterocyclyl or heterocyclyl-lower alkyl; the lower alkyl, cycloalkyl, lower alkenyl, cycloalkenyl, lower alkynyl, aryl-lower alkyl, aryl and the heterocyclyl moieties being unsubstituted or substituted with at least one group selected from carboxy, amino, aminoethyl, carbamoyl, nitro, cyano, lower alkyl, lower alkoxy, hydroxy, halogen and trifluoromethyl. The manufacturing method comprises the steps of: converting a phosphonium salt of the formula(II) into the corresponding ylide of the formula(III); reacting it with aldehyde of the formula(IV).