Synthesis of trifluoromethylated 2-azirines through Togni reagent-mediated trifluoromethylation followed by PhIO-mediated azirination.

Beilstein J Org Chem

Tianjin Key Laboratory for Modern Drug Delivery and High-Efficiency, School of Pharmaceutical Science and Technology, Tianjin University, Tianjin 300072, China.

Published: June 2018

The reaction of enamine compounds with the Togni reagent in the presence of CuI afforded β-trifluoromethylated enamine intermediates, which were converted directly to biologically interesting trifluoromethylated 2-azirines by an iodosobenzene (PhIO)-mediated intramolecular azirination in a one-pot process.

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Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6009194PMC
http://dx.doi.org/10.3762/bjoc.14.123DOI Listing

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