Late-Stage Functionalization: Total Synthesis of Beauveamide A and Its Congeners and Their Anticancer Activities.

Asymmetric total synthesis of cyclotetradepsipeptide beauveamide A has been achieved for the first time. A macrolactamization strategy involving two possible sites has been explored to find the most effective route for cyclization. A late-stage functionalization approach has been adopted for easy access of non-natural analogues of beauveamide A for further biological evaluation. Interestingly, the anticancer activity of one of the synthesized analogues was better than that of the parent natural product.