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Updated: Feb 26, 2026

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Photochemical Synthesis of DNA-Encoded 3H-Azepines via Skeletal Editing of Nitroarenes
Jia-Ying Xue1, Jia-Hui Shi1, Yuan Yao1
1Guangdong Provincial Key Laboratory of Chiral Molecules and Drug Discovery, State Key Laboratory of Anti-Infective Drug Discovery and Development, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China.
Abstract:
We report a skeletal editing strategy based on DNA-encoded nitroarenes for the direct conversion of benzene cores into valuable 3H-azepine scaffolds. This transformation is efficiently promoted by visible light in the presence of P(Oi-Pr)3, which serves as a reductant to generate reactive nitrene intermediates from the nitro group. Demonstrating broad substrate scope with applicability to pharmaceutical molecules, this protocol offers an efficient and versatile route to DNA-encoded 3H-azepine derivatives. It thus establishes a robust platform for skeletal diversification in DNA-encoded library synthesis.
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