Synthesis of Multicyclic β-Lactam Derivatives via Solid-Phase-Generated Ketenes

摘要

β-Lactams are arguably one of the most important heterocyclic skeletons irt organic chemistry. Because of their unique biological properties, β-lactam derivatives have been the object of intense investigation in synthetic and medicinal chemistry areas. Since the discovery of penicillin, a number of bicicylic β-lactams have found broad applicability in antibacterial therapy. Aside from penicillin analogues, many cephalosporins, carbapenems, oxapenams, etc., are also currently used as effective weapons in the fight against bacteria. More recently, the significance of β-lactams has reached new frontiers, mostly because of the discovery of derivatives that show biological activities such as inhibition of prostate specific antigen, thrombin, human cytomega-lovirus protein, human leukocyte elastase, cholesterol absorption, cysteine protease, and human fatty acid amide hydrolase; as well as neuroprotective action.