Synthesis of Isoxazole Triflones
Synthesis of Isoxazole Triflones
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DOI：
10.1002/ejoc.201101814
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发表时间：
2012-03
影响因子：
2.8
通讯作者：
Hiroyuki Kawai;Yutaka Sugita;Etsuko Tokunaga;N. Shibata
中科院分区：
文献类型：
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作者：
Hiroyuki Kawai;Yutaka Sugita;Etsuko Tokunaga;N. Shibata
首次实现了异恶唑三氟甲磺酰基异恶唑3（4-三氟甲磺酰基异恶唑，4-三氟甲基异恶唑）的合成。本发明的方法提供了具有生物吸引力的异恶唑，其特征在于在4-位上具有三氟甲磺酰基，在所有情况下具有良好至高产率的宽底物范围。
The first practical synthesis of isoxazole triflones 3 (4-trifluoromethanesulfonylisoxazoles, 4-triflylisoxazoles) has been achieved by an operationally simple procedure consisting of the reaction between readily available α-triflyl ketones 4 and imidoyl chlorides 5 in the presence of triethylamine. The present method provides the biologically attractive isoxazoles featuring a triflyl group at the 4-position with a wide substrate scope in good to high yield in all cases.