The first oxazolinyl‐assisted ruthenium(II)‐catalyzed direct C─H chalcogenations of 2‐aryloxazolines has been achieved. The reaction proceeds smoothly with high functional group tolerance and regioselectivity to afford the sulfur‐ and selenium‐containing oxazoline compounds. The chalcogenation products can be easily converted into bioactive chalcogenoxanthones and useful sulfoxide‐oxazoline ligands. This efficient methodology is applied to the late‐stage modification of pharmaceutical compounds.
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He et al. (2026) studied this question.
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