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| Thieme eJournals / Abstract | Contact Us |
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| Synlett 2005: 2209-2213
DOI: 10.1055/s-2005-872248 |
© Georg Thieme Verlag Stuttgart · New York
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Rapid Synthesis of Aryl Azides from Aryl Halides under Mild Conditions
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| 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
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Received
25 June 2005 |
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. Key words
copper - aryl azides - aryl halides - ligands - azidonation
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