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Efficient synthesis of substituted pyrazoles Via [3+2] cycloaddition catalyzed by lipase in ionic liquid
Process Biochemistry ( IF 3.7 ) Pub Date : 2022-12-02 , DOI: 10.1016/j.procbio.2022.11.020
Fengxi Li , Yaning Xu , Ciduo Wang , Chunyu Wang , Hanqing Xie , Yuelin Xu , Peng Chen , Lei Wang

In this work, an enzymatic method for the de novo construction of diverse substituted pyrazoles from readily available diazo compounds and alkynoates/allenoates in ionic liquids was established. Under the optimum reaction condition (3-alkynoates or allenoates (0.5 mmol), diazo compounds (0.6 mmol), [BMIM][PF6] (2 mL), C. rugosa lipase (15 mg), 45 °C, 8 h.), pyrazoles bearing different groups were obtained in satisfactory yields (61 %−93 %). The method features a diversity of substituents of the pyrazole products and remarkably simple work-up.



中文翻译:

离子液体中脂肪酶催化[3+2]环加成高效合成取代吡唑

在这项工作中,建立了一种酶促方法,用于从离子液体中容易获得的重氮化合物和炔酸/联烯酸从头构建各种取代的吡唑。在最佳反应条件下(3-alkynoates or allenoates (0.5 mmol), diazo compounds (0.6 mmol), [BMIM][PF 6 ] (2 mL), C. rugosa lipase (15 mg), 45 °C, 8 h .), 以令人满意的收率 (61 %−93 %) 获得了带有不同基团的吡唑。该方法的特点是吡唑产品的取代基多种多样,而且后处理非常简单。

更新日期:2022-12-02
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