PROCESS FOR PRODUCING CEPH-3-EME-4-CARBOXYLIC ACID DERIVATIVES

摘要

1472870 Cephalosporin synthesis SOC FARMACEUTICI ITALIA SpA 20 May 1975 [22 May 1974] 28410/76 Divided out of 1472865 Heading C2C A process for the preparation of a cephalosporin having the general formula comprises treating a thiohydrazoazetidine of the formula wherein R is hydrogen, (C 1 -C 4 )alkyl, cyanomethyl, thienylmethyl, furylmethyl, naphthylmethyl, benzyl, phenoxymethyl, phenylisopropyl, phenoxyisopropyl, 4 - pyridyl - 4 thiomethyl or 1-tetrazolyl-methyl; R2 and R3 represent (C 1 -C 4 )alkyl, a mononuclear aryl or heterocyclic group, cyano, -COR4, -COOR4, -PO(OR4) 2 or -CONHR4 in which R4 is (C 1 -C 4 )alkyl or a mononuclear aryl or heterocyclic group; or R2 and R3 together represent a residue of any of the formulae Y is a residue of the formula and Z is hydrogen, bromine, iodine, hydroxyl, alkanoyloxy, alkyloxy, azido, amino, acetoxy, carbamate or an S-mononuclear nitrogen heterocyclic ring with an organic or inorganic base or an inorganic basic or weakly acid oxide at a temperature of from -100‹ to + 120‹ C. The inorganic oxide is suitably Al 2 O 3 , Fe 2 O 3 , Cr 2 O 3 or SiO 2 , and the base is suitably Na 2 CO 3 , NH 4 OH an alkali or alkaline earth metal hydroxide, an alkali metal alcoholate, an aliphatic, aromatic or heterocyclic amine, an alkylammonium base or a basic resin.