We have devised an expeditious. efficient, asymmetric synthesis of the C(33
)-C(37) fragment of amphotericin B that proceeds in 14 steps and 16% overal
l yield from tiglic aldehyde ((E)-2-methylbut-2-enal) with complete stereoc
ontrol. The route described herein relies on the application of recently de
veloped methods in catalytic asymmetric synthesis for stereocontrol through
enantio- and diastereoselective functionalization of a substituted sorbate
derivative.