Microwave promoted amination of 3-bromoisoxazoles |
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| Authors: | Jane E. Moore Joseph P.A. Harrity |
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| Affiliation: | a Department of Chemistry, University of Sheffield, Brook Hill, Sheffield S3 7HF, UK
b Department of Medicinal Chemistry, Organon Laboratories Ltd., Newhouse, Lanarkshire ML1 5SH, UK |
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| Abstract: | This Letter describes the amination of 3-bromoisoxazoles by a nucleophilic aromatic substitution reaction. We have found 3-bromoisoxazoles to be inert to substitution under thermal conditions, however, the employment of phosphazene bases under microwave irradiation facilitates the amination process and allows the corresponding 3-aminoisoxazoles to be isolated in moderate yield. |
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| Keywords: | Isoxazoles Microwave irradiation BEMP Amination |
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