Direct C–H acylations and
carbamoylations of heterocycles
can now be readily achieved without requiring any conventional metal,
photocatalyst, electrocatalysis, or light activation, thus significantly
improving on sustainability, costs, toxicity, waste, and simplicity
of the operational procedure. These mild conditions are also suitable
for gram-scale reactions and late-stage functionalizations of complex
molecules, including pharmaceuticals, N,N-ligands, and light-sensitive molecules.
α,β-Unsaturated acyl ammonium species are versatile intermediates that have been applied in a variety of transformations including Michael additions, domino reactions and cycloadditions.
The photocatalytic generation of α-amino radicals is combined with chiral isothiourea derived α,β-unsaturated acyl ammonium intermediates. The reaction proceeds via a [3+2] radical-polar crossover mechanism to generate γ-lactams in good...
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