Patent ID: 6384212
Filing Date: 2002-05-07
Classification: C07D

Abstract:
A process for the preparation of cephalosporin antibiotics represented by the following formula (I), in which an acid addition salt of a crystalline aminothiazole compound represented by the following formula (II) is acylated by reaction with a 7-aminocephalosporanic acid derivative represented by the following formula (III) in a solvent: wherein R1 and R2 are the same or different and independently represent H, an alkyl group of 1 to 4 carbon atoms, or a cycloalkyl group of 3 to 5 carbon atoms, R4 represents acetoxymethyl, pyridiniummethyl, or vinyl, COOM is COOâˆ’ when R4 is pyridiniummethyl and COOH otherwise, X represents chlorine or bromine, and the acid in the acid addition salt represents an inorganic acid selected from the group consisting of hydrochloric acid, hydrobromic acid, sulfuric acid, and perchloric acid, or an organic acid selected from the group consisting of formic acid, acetic acid, trifluoroacetic acid, propionic acid, methanesulfonic acid, and benzenesulfonic acid.