2,2,2-Trifluoroethyl Formate: A Versatile and Selective Reagent for the Formylation of Alcohols, Amines, and N-Hydroxylamines
David R. Hill*, Chi-Nung Hsiao, Ravi Kurukulasuriya and Steven J. Wittenberger
*Abbott Laboratories, Global Pharmaceutical R&D, 1401 Sheridan Road, D-R450, Bldg. R8, North Chicago, Illinois 60064-4000, Email: david.hillabbott.com
D. R. Hill, C.-N. Hsiao, R. Kurukulasuriya, S. Wittenberger, Org. Lett., 2002, 4, 111-113.
DOI: 10.1021/ol016976d (free Supporting Information)
Various alcohols, amines and N-hydroxylamines gave corresponding formylated adducts in high yields by treatment with 2,2,2-trifluoroethyl formate (TFEF). Chemoselective formylation of a primary amine could be readily achieved in the presence of an unprotected primary alcohol.
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