Penicillins and their production

Details Penicillins and their production Penicillins and their production

C - Chemistry, Metallurgy

07

D

260/114.1

C07D 499/12 (2006.01) C07D 215/56 (2006.01) C07D 221/04 (2006.01) C07D 239/557 (2006.01) C07D 499/00 (2006.01) C07D 499/72 (2006.01)

Patent

CA 1049504

PENICILLINS AND THEIR PRODUCTION Abstract of the Disclosure Penicillins of the formula: Image (IA) wherein Image is a six-membered heteroaromatic ring containing 1 or 2 hetero nitrogen atoms, R is phenyl, p-hydroxyphenyl, C1-C4 alkyl, cyclohexadienyl, thienyl or isothiazolyl, Y is hydrogen, lower alkanoyl or lower alkoxycarbonyl and R1 and R2 are each hydrogen, lower alkyl, lower alkanoyl, benzoyl, lower alkylmercapto, hydroxyl, mercapto, hydroxy(lower)alkyl, halogen or cyano or R1 and R2 linked together represent a lower alkylene chain optionally substituted with an oxo group, and non-toxic, pharmaceutically acceptable salts thereof are prepared by reacting a compound of the formula: Image wherein R is as defined above, or a derivative thereof, with a carboxylic acid of the formula: Image wherein Image , Y, R1 and R2 are each as defined above, or a reactive derivative thereof, if necessary, followed by hydrolysis or acylation of the resulting product and/or elimination of a protective group. The novel penicillins exhibit antimicrobial activity against various gram positive and gram-negative bateria including Pseudomonas.

166058

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