Reported herein an unprecedented 1,2-azide migratory hydroazidation and subsequent -difluorination of alkynes accessing β-difluorinated alkyl azides. Importantly, functional group controlled 1,2-azide or 1,2-aryl migration was observed in the case of aromatic alkynes. Moreover, the azide group is sustained up to the final product. The method can be easily adapted for large-scale preparation, and the resulting products can be readily transformed into -difluoro group containing amine and triazole derivatives.
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http://dx.doi.org/10.1021/acs.orglett.9b03593 | DOI Listing |
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