Microwave-assisted reaction creates new heteroaromatic amino acids from histidine derivatives, suggesting diverse applications.
We report a regioselective, microwave‐assisted Pd‐catalyzed intramolecular C─H (hetero)arylation of histidine and its derivatives. The one‐step transformation enables access to ring‐annulated tri‐ and tetracyclic α‐amino acids by selectively functionalizing the imidazole side‐chain ring at C‐5. This strategy demonstrates applicability across protected histidine and its derivatives by constructing π‐extended, conformationally rigid α‐amino acids and related heterocycles.
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Rao et al. (2026) studied this question.
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