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Issue 8, 2019
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Oxidative C(sp3)–H functionalization of methyl-azaheteroarenes: a facile route to 1,2,4-triazolo[4,3-a]pyridines

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Abstract

We herein describe an oxidative [4 + 1] annulation used to prepare 1,2,4-triazolo[4,3-a]pyridines in the presence of I2–DMSO. This protocol enables synthesis of triazolo[4,3-a]pyridine–quinoline linked diheterocycles via a direct oxidative functionalization of sp3 C–H bonds of 2-methyl-azaheteroarenes. The reaction shows a wide substrate scope and good functional group tolerance.

Graphical abstract: Oxidative C(sp3)–H functionalization of methyl-azaheteroarenes: a facile route to 1,2,4-triazolo[4,3-a]pyridines

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Publication details

The article was received on 06 Jan 2019, accepted on 23 Jan 2019 and first published on 23 Jan 2019


Article type: Communication
DOI: 10.1039/C9OB00033J
Citation: Org. Biomol. Chem., 2019,17, 2087-2091

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    Oxidative C(sp3)–H functionalization of methyl-azaheteroarenes: a facile route to 1,2,4-triazolo[4,3-a]pyridines

    W. Weng, Y. Gao, X. Zhang, Y. Liu, Y. Shen, Y. Zhu, Y. Sun, Q. Meng and A. Wu, Org. Biomol. Chem., 2019, 17, 2087
    DOI: 10.1039/C9OB00033J

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