Process development and scale-up of cefotetan synthesis

Abstract

Cefotetan (YM09330) is a semi-synthetic injectable antibiotic which was discovered and developed by Yamanouchi Pharmaceutical Co., Ltd. and has been on the market since 1983. This compound shows a strong and wide spectrum of antibacterial activity and high stability against β-lactamase. This paper outlines the optimization of the synthetic process, the replacement of the trifluoroacetic acid used for the cleavage method of benzhydryl ester, work on the stability of diphenyldiazomethane, an alternative synthetic route to Cefotetan, the method for synthesizing the isothiazole derivative and the scale-up of Cefotetan synthesis.