Process for the conversion of 6-aminopenicillanic acid (6-APA) in 7-aminodesacetoxycephalosporanic acid (7-ADCA)

摘要

A process consisting in reacting one mole of an alpha-halobenzyl penicillin-(s)-sulphoxide with at least two moles of 3-trimethylsilyl-2-oxazolidinone (TMSO) at a temperature of between 60 and 120 DEG C in acetonitrile solution in the presence of a tertiary organic base p-toluene sulphonate and thiourea is described. The solvent is removed by evaporation from the solution obtained, the residue is diluted with water, the pH is adjusted to 4.2 and 7-aminodesacetoxycephalosporanic acid (7-ADCA) is isolated.