Morpholine derivatives as antibacterial agents

Details Morpholine derivatives as antibacterial agents Morpholine derivatives as antibacterial agents

C - Chemistry, Metallurgy

07

D

260/244.7

C07D 498/04 (2006.01) C07D 205/085 (2006.01) C07D 257/04 (2006.01) C07D 317/30 (2006.01)

Patent

CA 1095908

Abstract of the Disclosure The specification discloses a steroselective total synthesis of certain novel substituted Image 2'3-1, 4-morpholine-2carboxylic acids possessing a fused .beta.-lactam ring in the 1,6-position and carrying a substituent cis to carbon 5 in the 7-position of the fused ring system represented by the general formula Image wherein X is amino, azido or acylamido and Z represents optionally substituted C1-C6 alkyl, aryl, aralkyl or heterocyclic. When X is acylamino, these acids (and their pharmaceutically acceptable salts and physiologically hydrolyzed esters) are potent antibacterial agents. The compounds having the above general formula represent a new family of .beta.-lactam antibiotics. They can be considered nuclear analogs of cephalosporins in which the sulphur atom of the dihydrothiazine ring is replaced by an oxygen atom and shifted from position 5 to position 4 of the .beta.-lactam ring system as numbered in the formula above.

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