Journal
ORGANIC LETTERS
Volume 21, Issue 12, Pages 4808-4811Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.orglett.9b01697
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Funding
- National Natural Science Foundation of China [21472137, 21532008, 21772142]
- National Basic Research Program of China [2014CB745100]
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A silver-catalyzed regioselective [3 + 2] cycloaddition reaction of PhSO2CF2CHN2 with aryl diazonium salts is described. This protocol enables the straightforward construction of a novel class of difluoromethylated tetrazoles under mild conditions, tolerates a broad spectrum of functionalities, and is applicable to one-pot operation from commercially available aniline derivatives. The synthetic merit of this method is further demonstrated by the facile preparation of versatile difluoromethylated azoles, including a valuable HCF2-analogue of P2X3 receptor antagonist.
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