4.7 Article

Diverse Trifluoromethyl Heterocycles from a Single Precursor

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JOURNAL OF ORGANIC CHEMISTRY
卷 77, 期 3, 页码 1396-1405

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AMER CHEMICAL SOC
DOI: 10.1021/jo202201w

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  1. EPSRC
  2. GlaxoSmithKline

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Ethyl 2-diazo-4,4,4-trifluoro-3-oxobutanoate is a highly versatile intermediate for the synthesis of a wide range of trifluoromethyl heterocycles. With the use of rhodium(II) or copper(II) catalyzed carbene X-H insertion reactions as key steps, a diverse set of trifluoromethyl-oxazoles, -thiazoles, -imidazoles, -1,2,4-triazines, and -pyridines are available from the diazoketoester, either directly in a single step or with just one additional step.

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