PROCESSES FOR THE PREPARATION OF beta -LACTAM DERIVATIVE

摘要

A process for the preparation of an allenyl- beta -lactam compound which comprises reacting the hydroxyl group of a beta -lactam compound of general formula (1) with a reactive functional derivative of a sulfonic acid of the general formula (2): R<5>-SO2-X to form a beta -lactam compound of general formula (3) and reacting the formed compound with a basic anion-exchange resin containing a tertiary organic base immobilized thereon to attain the preparation of an allenyl- beta -lactam compound of general formula (4) and the stable isolation thereof from the reaction mixture in a high yield at a high purity. Another process for the preparation of an allenyl- beta -lactam compound which comprises reacting the hydroxyl group of a beta -lactam compound of general formula (1) with a reactive functional derivative of a sulfonic acid of the general formula (2): R<5>-SO2-X to form a beta -lactam compound of general formula (3), reacting the formed compound with a tertiary organic base to form an allenyl- beta -lactam compound of general formula (4) and treating the resulting reaction mixture with both an acidic cation-exchange resin and a basic anion-exchange resin either alternately or simultaneously to isolate the compound of general formula (4) from the reaction mixture stably. A process of preparing a 3-halocephem derivative of general formula (6) by reacting an allenyl- beta -lactam compound of general formula (4) with a halogenating agent in the presence of a sulfinate or thiolate ion scavenger.