Efficient trifluoromethylation of C(sp2)–H functionalized α-oxoketene dithioacetals: a route to the regioselective synthesis of functionalized trifluoromethylated pyrazoles

N. Sharma; N. Kumari; T. S. Chundawat; S. Kumar; S. Bhagat

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Efficient trifluoromethylation of C(sp2)–H functionalized α-oxoketene dithioacetals: a route to the regioselective synthesis of functionalized trifluoromethylated pyrazoles

机译：C（sp 2 ）– H官能化的α-氧杂环丁烯二硫缩醛的有效三氟甲基化：官能化三氟甲基化吡唑区域选择性合成的途径

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An operationally simple approach for the regioselective construction of diversely substituted trifluoromethylated pyrazoles via nucleophilic trifluoromethylation of iodo-substituted α-oxoketene dithioacetals is described. X-ray crystallographic studies confirmed the trifluoromethylation as well as formation of a regioselective cyclized product. Furthermore, trifluoromethylated pyrazoles bearing thiomethyl groups may allow further functionalization and are of considerable interest in medicinal chemistry.

机译：描述了一种操作简单的方法，用于通过碘取代的α-氧杂环丁烯二硫缩醛的亲核三氟甲基化来选择性地构建不同取代的三氟甲基化的吡唑。 X射线晶体学研究证实了三氟甲基化以及区域选择性环化产物的形成。此外，带有硫代甲基的三氟甲基化的吡唑可以允许进一步的官能化，并且在药物化学中具有相当大的意义。

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《RSC Advances》 |2017年第17期|共4页
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N. Sharma; N. Kumari; T. S. Chundawat; S. Kumar; S. Bhagat;
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Efficient trifluoromethylation of C(sp2)–H functionalized α-oxoketene dithioacetals: a route to the regioselective synthesis of functionalized trifluoromethylated pyrazoles

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