Synthesis of 3-Aminoisoxazoles via the Addition−Elimination of Amines on 3-Bromoisoxazolines
摘要:
A novel two-step procedure for the synthesis of 3-amino-5-substituted-isoxazoles Is described. In the presence of a base, readily available 3-bromoisoxazolines react with amines to afford 3-aminoisoxazolines. An oxidation protocol was developed for these heterocycles to provide 3-aminoisoxazoles in consistently high yield.
Synthesis of 3-Aminoisoxazoles via the Addition−Elimination of Amines on 3-Bromoisoxazolines
作者:Mélina Girardin、Pamela G. Alsabeh、Sophie Lauzon、Sarah J. Dolman、Stéphane G. Ouellet、Greg Hughes
DOI:10.1021/ol9000284
日期:2009.3.5
A novel two-step procedure for the synthesis of 3-amino-5-substituted-isoxazoles Is described. In the presence of a base, readily available 3-bromoisoxazolines react with amines to afford 3-aminoisoxazolines. An oxidation protocol was developed for these heterocycles to provide 3-aminoisoxazoles in consistently high yield.