Synlett 2005(14): 2209-2213  
DOI: 10.1055/s-2005-872248
LETTER
© Georg Thieme Verlag Stuttgart · New York

Rapid Synthesis of Aryl Azides from Aryl Halides under Mild Conditions

Jacob Andersena, Ulf Madsenb, Fredrik Björklinga, Xifu Liang*a
a Department of Medicinal Chemistry, LEO Pharma, Industriparken 55, 2750 Ballerup, Denmark
Fax: +45(7226)3320; e-Mail: xifu.liang@leo-pharma.com;
b Department of Medicinal Chemistry, The Danish University of Pharmaceutical Sciences, 2100 Copenhagen, Denmark
Further Information

Publication History

Received 25 June 2005
Publication Date:
26 July 2005 (online)

Abstract

A rapid synthesis of aryl azides from the corresponding aryl halides catalyzed by CuI/diamine is described. Sodium ascorbate was found to have a positive effect on stabilization of the catalyst system. The reactions were performed under very mild conditions generally with high yields. In the case of aryl iodides, the transformation could be carried out at room temperature.