Synthesis of (+)-Agelastatin A

Significance

An inhibitor of glycogen synthase kinase-3b, Agelastatin A provides a potential new treatment for Alzheimer’s disease. Noteworthy in this approach are (1) the use of both intra- and intermolecular palladium-catalyzed asymmetric allylic alkylation (AAA) reactions wherein the use of pyrrole and N-methoxyamide nucleophiles are disclosed, and (2) the aziridination of an olefin mediated by NHC-copper complex G.