Synthesis of Indole-Derived Fluorine-Containing Amino Acids

Hannah C. Cade, Mark Blocker, Abid Shaikh

Department of Chemistry, Georgia Southern University, 521 College of Education Drive, Statesboro, GA 30460-8064, USA


A Brønsted acid promoted direct aminoalkylation of various indoles with trifluoromethyl oxazolidine is described. A catalytic amount of triflic acid provided straightforward access to the corresponding trifluoromethyled amino esters under mild reaction conditions and a short reaction time of 4 h. On further hydrogenolysis and hydrolysis of ester, the synthesis of indole derived unnatural trifluoromethylated amino acids was achieved. Journal of Nature and Science, 1(8):e169, 2015

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