W. Wenfeng
2010
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Journal
Chinese Journal of Pharmaceuticals
Abstract
Cefbuperazone was synthesized from 4-ethyl-2,3-dioxopiperazine by chlorination with triphosgene,condensation with D-threonine,oxidation with formic acid and chlorination with oxalyl chloride to give 2-[(4-ethyl-2,3-dioxopiperazin-1-carbonyl)amino]-3-formyloxybutyryl chloride,which was subjected to condensation with diphenylmethyl 7β-amine-7α-methoxy-3-[(1-methyl-1H-tetrazol-5-ylthio)methyl]-8-oxo-5-thio-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate(7-MAC) followed by deprotection of diphenylmethyl group and formyl group. The total yield was about 5%.