Cephalosporins, processes for producing the same,...

C - Chemistry – Metallurgy – 07 – D

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C07D 501/18 (2006.01) C07D 241/18 (2006.01) C07D 405/04 (2006.01)

Patent

CA 1276139

ABSTRACT OF THE DISCLOSURE Intermediates in the production of cephalosporins in which a substituted or unsubstituted 2,3-dioxo-1,2,3,4-tetra- hydropyrazinyl, 2-oxo-1,2-dihydropyrazinyl, 3,6-dioxo-1,2,3,6- tetrahydropyridazinyl or 6-oxo-1,6-dihydropyridazinyl group is attached to the exomethylene group at the 3-position of the cephem ring through a carbon-nitrogen bond and which have the following group atached to the amino group at the 7-position: Image wherein -A- represents a group of the formula, -CH2- or a group of the formula, Image in which R18 represents a hydrogen atom or a sutstituted or unsubstituted alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, aralkyl, aryl, hererocy- clic group or a hydroxyl-protecting group or a group of the formula, Image (each of R19 and R20, which may be the same or different, represents a hydroxyl, alkyl, aralkyl, aryl, alkoxy, aralkyloxy or aryloxy group), and the bond Image means that the compound may be a syn-isomer or an anti-isomer or a mixture thereof; R4 represents a hydrogen atom or a halogen atom; and R5 represents a hydrogen atom or a protected or unprotected amino group. These cephalosporins have a braod antibacterial spectrum, are stable against .beta. -lactamase pro- duced by bacteria, have a low toxicity, and are well absorbed when administered orally or parenterally.

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