Synthesis of Bryostatin Analogues

Significance

Bryostatin 1 is a potent antineoplastic agent that restores apoptotic function, stimulates the immune system and reverses multidrug resistance through its modulation of protein kinase C (PKC). It also enhances cognition and memory in animals. Only 1.5 mg of bryostatin 1 is needed for an eight-week clinical treatment cycle. The Wender group’s synthesis of the simpler analogue depicted features an exceptionally efficient Prins-driven macrocyclization that is one of the most complex examples of any Prins cyclization.