We herein report a metal-free, innate, and practical C–H formylation of nitrogen heterocycles using trioxane as the formyl equivalent. Notably, this reaction provides a mild and robust strategy for modifying medicinally relevant heterocycles. Based on preliminary computational studies, we uncover a correlation between C–H bond dissociation enthalpy and the site of formylation.

Metal- and acid-free C–H formylation of nitrogen heterocycles

255th National Meeting (2018)

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