4.8 Article

Catalyst-Free Regioselective N2 Arylation of 1,2,3-Triazoles Using Diaryl Iodonium Salts

Journal

ORGANIC LETTERS
Volume 21, Issue 16, Pages 6255-6258

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/acs.orglett.9b02140

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Funding

  1. Loker Hydrocarbon Research Institute

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The widespread application of 1,2,3-triazoles in pharmaceuticals has resulted in substantial interest toward developing efficient postmodification methods. Whereas there are many postmodification methods available to obtain N-1-substituted 1,2,3-triazoles, developing a selective and convenient protocol to synthesize N-2-aryl-1,2,3-triazoles has been challenging. We report a catalyst-free and regioselective method to access N-2-aryl-1,2,3-triazoles in good to excellent yields (66-97%). This scalable postmodification protocol is effective for a wide range of substrates.

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