C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
260/108
C07D 501/18 (2006.01) A61K 31/43 (2006.01) A61K 31/545 (2006.01) C07D 499/00 (2006.01) C07D 501/10 (2006.01) C07D 501/60 (2006.01)
Patent
CA 1056816
ABSTRACT OF THE DISCLOSURE The present invention relates to a process for the conversion of 6-aminopenicillanic acid (6-APA) to 7-aminodesacetoxycephalosporanic acid (7-ACDA), the improvement comprises reacting one mole of a compound selected from the group consisting of alpha-chloro- and alpha-bromobenzyl penicillin-(s)-sulphoxide with from two to four moles of 3-trimethylsilyl-2-oxazolidinone (TMSO) at a temperature of between 60° and 120°C in an inert non-hydroxylic solvent and in the presence of thiourea and a compound selected from the group consisting of triethylamine, dimethylaniline, quinoline and picoline p-toluene sulfonate to obtain a solution, thereafter removing the solvent by evaporation, diluting the residue with water, adjusting the pH to 4.2, and isolating 7-amido- desacetoxycephalosporanic acid (7-ADCA).
238601
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