Preparation of cephalosporins

Details Preparation of cephalosporins Preparation of cephalosporins

C - Chemistry, Metallurgy

07

D

260/104, 260/101

C07D 501/20 (2006.01) C07D 277/48 (2006.01)

Patent

CA 1240985

Abstract of the Disclosure Highly active substantially pure z-isomers of cephalo- sporins of the formula: Image (I) (in which R1 denotes alkyl, cycloalkyl, aryl or heterocyclic radical, and X denotes hydrogen, alkyl, halogen, alkoxy, hydroxy- methyl, formyloxymethyl, alkylcarbonyloxymethyl, aminocarbonyloxymethyl, pyridinium methyl, 4-carbamoylpyridinium methyl or heterocyclylthio- methyl) are produced by reacting corresponding Z-isomers of the formula: Image (XVI) (in which R2 denotes -CO2R3 or hydrogen, R3 denotes alkyl, cycloalkyl, alkenyl, cycloalkenyl aryl or heterocyclic radical, and R5 denotes alkyl, alkenyl, cycloalkyl, cycloalkenyl, carbocyclic or heterocyclic aryl or heterocyclic radical) with a cephalosporanic acid of the formula: Image (XVII) and splitting of the group -CO2R3 of present. The intermediate Z-isomers (XVI) may be produced by reacting Z-isomer acids of the formula: Image (XIII) with a compound of the formula: Z-SO2-R5 (in which Z denotes Cl, Br or O-SO2-R5).

541405

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