C3-Cyanation of Pyridines: Constraints on Electrophiles and Determinants of Regioselectivity,Angewandte Chemie International Edition

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C3-Cyanation of Pyridines: Constraints on Electrophiles and Determinants of Regioselectivity
Angewandte Chemie International Edition ( IF 16.1 ) Pub Date : 2022-12-14 , DOI: 10.1002/anie.202216894
Ming Zhang ₁ , Qingyang Zhou ₂ , Heng Luo ₁ , Zi-Lu Tang ₁ , Xiufang Xu ₂ , Xiao-Chen Wang ₁

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C3-selective cyanation of pyridines was accomplished by a tandem process of borane-catalyzed pyridine hydroboration, substitution of the resulting dihydropyridine with a cyano electrophile, and finally oxidative aromatization. This method was suitable for use in late-stage cyanation of pyridine drugs.

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