Facile approach to optically active alpha-alkylidene-beta-amino esters by thermal Overman rearrangement

Org Lett. 2010 Jul 16;12(14):3234-7. doi: 10.1021/ol1011746.

Abstract

A convenient synthetic method for enantioenriched (E)-alpha-alkylidene-beta-amino esters has been developed through thermal Overman rearrangement. Readily accessible (Z)-beta-branched Morita-Baylis-Hillman esters serve as chiral pool precursors. Thermal rearrangement proceeded through a concerted pseudopericyclic transition state to produce (E)-stereoselective products. We expanded the synthetic utilities of alpha-alkylidene-beta-amino esters via preparation of alpha-alkylidene-beta-lactam derivatives.