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Investigation of the scope of a [3+2] cycloaddition approach to isoxazole boronic esters |
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| Authors: | Jane E. Moore Katharine M. Goodenough Mark York Joseph P.A. Harrity |
| Affiliation: | a Department of Chemistry, University of Sheffield, Sheffield S3 7HF, UK b Department of Chemistry, Organon Laboratories Ltd, Newhouse, Lanarkshire ML1 5SH, UK c Neurology and GI Center of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK |
| Abstract: | The [3+2] cycloaddition reaction of nitrile oxides and alkynylboronates provides direct access to a wide variety of isoxazole boronic esters. Specifically, this technique has been employed to generate trisubstituted isoxazole 4-boronates and disubstituted isoxazoles where the boronic ester moiety can be installed at C-4 or C-5 with high levels of regiocontrol. The application of this methodology in the synthesis of non-steroidal antiinflammatory agents is also described. |
| Keywords: | Cycloadditions Boronic esters Isoxazoles Regioselective |
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