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One-Pot Synthesis of CF3-Substituted Pyrazolines/Pyrazoles from Electron-Deficient Alkenes/Alkynes and CF3CHN2 Generated in situ: Optimized Synthesis of Tris(trifluoromethyl) pyrazole

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EUROPEAN JOURNAL OF ORGANIC CHEMISTRY
卷 2014, 期 12, 页码 2487-2495

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WILEY-V C H VERLAG GMBH
DOI: 10.1002/ejoc.201301852

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Synthetic methods; Nitrogen heterocycles; Fluorine; Multicomponent reactions; Cycloaddition

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The [3+2] cycloaddition of CF3CHN2, generated in situ, with electron-deficient alkenes/alkynes affords CF3-substituted pyrazolines/pyrazoles in quantitative yields. The one-pot three-component reaction between CF3CH2NH2HCl, NaNO2, and the substrate proceeds at room temperature in dichloromethane/water.

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