Abstract
Based on the consideration that biologically active chiral compounds should be prepared in optically active forms which show desired biological activities, the compounds not only exhibiting interesting biological activities but also bearing intriguing structures were selected as synthetic targets and their efficient syntheses were studied by employing optical resolution, asymmetric synthesis and chemical transformation. Thus, efficient syntheses of the anticancer agents such as anthracyclines, nogalamycins, and sesbanimides were accomplished in optically active forms. Syntheses of optically active quinocarcin and fredericamycin A showing pronounced anticancer activities were also studied. A number of efficient synthetic routes to the optically active key intermediates of antibacterial carbapenem antibiotics and antihypertensive peptide-like renin inhibitors were successfully explored.
