Penicillin compounds and process for preparation thereof

Details Penicillin compounds and process for preparation thereof Penicillin compounds and process for preparation thereof

C - Chemistry, Metallurgy

07

D

260/114.1

C07D 499/70 (2006.01) C07D 471/04 (2006.01) C07D 499/00 (2006.01)

Patent

CA 1102311

ABSTRACT OF THE DISCLOSURE A penicillin compound of the formula Image wherein R is a formyl or acetyl group, and a nontoxic pharmaceutically ac- ceptable salt thereof. The penicillin compound is prepared by (A) reacting a compound of the formula Image or its salt or its reactive derivative at the carboxyl group, with 6-.alpha.- amino-p-hydroxybenzylpenicillin or its salt or its derivative, or reacting a compound of the formula Image or its salt or its reactive derivative at the carboxyl group, with 6-amino- penicillanic acid or its salt or its derivative, (b) optionally hydrolyzing or catalytically hydrogenolyzing the reaction product, and (e) optionally converting the reaction product to a nontoxic pharmaceutically acceptable salt. The penicillin compound has low toxicity and superior antibacterial activity especially against bacteria of the genus Pseudomonas and is suit- able for parenteral administration, especially for an intramuscular, intra- venuous or subcutaneous injection.

281637

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