PROCESS FOR PREPARING CEPHALOSPORIN COMPOUND USING RESPONSIVE PHOSPHATE DERIVATIVES OF THIASOL ACETATE

PURPOSE: Provided is a process for preparing cephalosporin compound useful as an antibiotics which can prepare a high level of cephem derivative represented by formula (I) with a high yield, using responsive phosphate derivatives of thiazol acetate represented by formula (II). CONSTITUTION: The process for preparing a cephem derivative (I) represented by scheme (2) is characterized by comprising an acylation of the responsive phosphate derivative of thiazol acetate and 7-aminocephalosporanic acid (7-ACA) derivative represented by formula (III) in an alcohol solvent in the presence of a base, wherein R1 is a carboxyl group or a protection carboxyl group and forms a salt of -COO-M+ with alkali metal (M+), or when R2 has a positive-charged substituent such as pyridinium, then R1 is COO-; R2 is hydrogen, methyl, vinyl, methoxymethyl, acetyloxymethyl, heterocyclicmethyl or heterocyclicthiomethyl group and may independently be substituted with a suitable substituent; R3 is hydrogen, methyl or C(Ra)2CO2Rb (wherein, Ra is hydrogen or methyl group and Rb is carboxyl protection group); R4 represents C1-C4 alkyl or phenyl, or forms 5- to 6-membered ring with an oxygen and phosphorus atoms; Q is N or CH.