Synthese von 3‐α‐Chlorvinylcephalosporinen

Abstract

Von 7‐Aminocephalosporansäure (7‐ACS) ausgehend werden die 3‐α‐Chlorvinylcephalosporine 6, 7, 8, 9, 10 und 11 synthetisiert. 6, 7, 8, 9 und 10 sind Zwischenstufen für die neue antibakterielle Verbindung 11. Das Produkt 6 erhält man aus Acetylcephalosporin 5 und Triphenylphosphin in CCl4.

Properties and Synthetic Utility ofN-Substituted Benzotriazoles

“…1-(Methylsulfonyl)-6-(trifluoromethyl)benzotriazole has been successfully used as an activating agent for the multistep synthesis of antibacterial cephalosporines …”

“…368 1-(Methylsulfonyl)-6-(trifluoromethyl)benzotriazole has been successfully used as an activating agent for the multistep synthesis of antibacterial cephalosporines. 370 The benzotriazole group in 1-(phenylsulfonyl)benzotriazole (for preparation, see section II.A.2) is readily displaced by amines and phenols allowing the preparation of benzenesulfonamides 1011 and benzenesulfonates 1012 in good yields 371 (Scheme 312).…”