A Formal Enantioselective Total Synthesis of FR901483

Abstract

A formal enantioselective total synthesis of the potent immunosuppressant FR901483 (<b>1</b>) has been accomplished. Our approach features the use of chiron <b>6</b> as the starting material, the application of the one-pot amide reductive bisalkylation method to construct the chiral aza-quaternary center (dr = 9:1), regio- and diastereoselective intramolecular aldol reaction to build the bridged ring, and ring closing metathesis to form the 3-pyrrolin-2-one ring