NEW PENICILLANIC ACID DERIVATIVE* ITS OPTICALLY ACTIVE ISOMER* ITS SALT* AND ITS PREPARATION

摘要

NEW MATERIAL: A penicillanic acid derivative of formula I (R<1>=phenyl, heterocyclic, pyridylthio; R<2>=H, alkali metal, ammouium, organic base cation, carboxyl protecting group), its optically active isomer, or its salt. EXAMPLE:Sodium 6-[3'-hydroxy-2'-(1H-tetrazol-1-yl)propionamide] penicillanate. USE:Anti-microbial agents, effective against gram negative (positive) bacteria. PROCESS:6-Aminopenicillanic acid of formula II or its derivative is made to react with 3-hydroxy-2-substituted propionic acid derivative of formula III (R<3>=H, alcohol protecting group) or its reactive derivative. Then, when R<3> is an alcohol protecting group, the protecting group is removed, and when R<2> is a carboxyl protecting group, the protecting group is removed if necessary. And if desired, the mixture is then subjected to the optical resolution and/or converted to the salt to give the compound of formula I, its stereoisomer and its salt.