Slicing and Splicing of Bromodifluoro--arylacetamides: Dearomatization and Difunctionalization of Pyridines.

Org Lett

Tianjin Key Laboratory of Molecular Optoelectronic Science, Department of Chemistry, School of Science, Tianjin University, Tianjin 300072, P. R. China.

Published: August 2020

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Article Abstract

Copper-catalyzed dearomatization and difunctionalization of pyridines have been disclosed, in which bromodifluoro--arylacetamide was sliced into five fragments and three or four of them were transferred to pyridine partners. Through this reaction, novel -difluoromethyl-2-imine dihydropyridine derivatives can be conveniently accessed from commercially available 4-amino substituted pyridines. This strategy demonstrates a novel fluorination method featuring high atom economy, environmental friendliness, an easily available catalyst, and simple operation.

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http://dx.doi.org/10.1021/acs.orglett.0c02368DOI Listing

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