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Stereocontrolled synthesis and alkylation of cyclic β-amino esters: asymmetric synthesis of a (−)-sparteine surrogate†‡
Jean-Paul R. Hermet,Aurélien Viterisi,Jonathan M. Wright,Matthew J. McGrath,Peter O'Brien,Adrian C. Whitwood,John Gilday
Organic & Biomolecular Chemistry Pub Date : 10/02/2007 00:00:00 , DOI:10.1039/B712503H
Abstract

A convenient method for the stereoselective synthesis of cyclic β-amino esters from an iodo αβ-unsaturated ester and α-methylbenzylamine is described. Subsequent enolate generation and alkylation proceeds with complete stereocontrol, with the two stereogenic centres working together. In this way, a functionalised piperidine suitable for alkaloid natural product synthesis was prepared. The usefulness of the methodology is exemplified with the concise synthesis of a (−)-sparteine surrogate.

Graphical abstract: Stereocontrolled synthesis and alkylation of cyclic β-amino esters: asymmetric synthesis of a (−)-sparteine surrogate
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