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A novel approach synthesizes axially chiral isoquinolinones in mild conditions, suggesting new pathways for heterobiaryl synthesis.
Herein, we report the successful implementation of a de novo isoquinolinone formation strategy for the atroposelective synthesis of isoquinoline-and pyridine-based axially chiral heterobiaryls. The construction of the isoquinolinone framework is achieved through a nickel/BOX complex-catalyzed, redox-neutral regio-and enantioselective [2+4] annulation between isoquinolinyl-or pyridinyl-substituted alkynes and oiodobenzamides. This protocol provides a straightforward and enantioselective approach to heterobiaryl atropisomers under mild reaction conditions.
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Wang et al. (2026) studied this question.
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