Process for P-nitrobenzyl ester cleavage in cephalosporin

Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...

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540219, C07D50104

Patent

active

055368301

ABSTRACT:
A process for converting cephalosporin p-nitrobenzyl ester (Formula I) to the corresponding cephalosporin free acid (Formula II) comprising treating the cephalosporin p-nitrobenzyl ester with a metal selected from the group consisting of iron, magnesium, aluminum, and tin, and with hydrochloric acid in a mixture of water and a water-miscible organic solvent. Preferably, the metal is iron in the form of a fine powder, and the reaction is carried out at a temperature in the range of 30.degree.-50.degree. C.

REFERENCES:
patent: 3781282 (1973-12-01), Garbrecht
patent: 3799924 (1974-03-01), Jackson
patent: 3925372 (1975-12-01), Chauvette
"Chemistry of Cephalosporin Antibiotics. XXIX 3-Halo- and 3-Methoxy-3-cephems", Journal of the American Chemical Society, 96:15, Jul. 24, 1974, pp. 4986-4987.

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