Synthesis 2006(19): 3199-3208  
DOI: 10.1055/s-2006-950226
PAPER
© Georg Thieme Verlag Stuttgart · New York

Phosphorus-Derived Chiral Auxiliaries for α-Alkylation of Secondary Amines by Anodic Oxidation

Emma Sierecki, Serge Turcaud, Thierry Martens*, Jacques Royer
‘Synthèse et structure de molécules d’intérêt pharmacologique’, UMR 8638 CNRS-Université René Descartes, Faculty of Pharmacy, 4 avenue de l’Observatoire, 75270 Paris Cedex 06, France
Fax: +33(1)43291403; e-Mail: thierry.martens@univ-paris5.fr;
Further Information

Publication History

Received 23 March 2006
Publication Date:
04 September 2006 (online)

Abstract

Chiral phosphorus-based structures were investigated as N-activating groups for anodic oxidation and as chiral inductors. This first study presents the results obtained for pyrrolidine, with allyltrimethylsilane as a standard nucleophile. The methoxylated compounds were obtained in excellent yields (82-98%). The dia­stereoselectivity of the alkylation step (18-66%) is discussed with regard to the chiral auxiliary.