Synthesis ot Brefeldin A Lactam Analogue

(+)-Brefeldin A (1) has been, since its isolation1 and structural elucidation2 many years ago, one of the most attractive targets for synthetic chemists due to its wide range of biological activities and well-functionalized macrolide structure. Its biological mode of action has been disclosed by a number of important discoveries. Especially the ability of brefeldin A to induce DNA fragmentation associated with apoptosis in cancer cells has stimulated a great deal of recent interest in its preclinical development as an anticancer agent. (omitted)