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Updated: May 3, 2026

Protocol for the Synthesis of Ortho-trifluoromethoxylated Aniline Derivatives
Published on: January 19, 2016
Trifluoromethylated heterocycles
Andrei A Gakh, Yuriy Shermolovich1
1Oak Ridge National Laboratory, Oak Ridge, TN 37831, USA, The University of Virginia, Charlottesville, VA 22908, USA, The Discovery Chemistry Project, Bethesda, MD 20824, USA. gakhaa@yahoo.com.
Abstract:
This review is a follow-up to the previous chapter, "Monofluorinated Heterocycles" (Topics in Heterocyclic Chemistry, 2012, 33-63), and presents an overview of synthetic chemistry of heterocycles with only one trifluoromethyl group directly attached to the ring (trifluoromethylated heterocycles). Particular attention is given to the modern direct trifluoromethylation methods, including catalytic reactions, organometallic reagents, carbene and hypervalent chemistry, utilization of ionic nucleophilic and electrophilic trifluoromethylating agents, and to other pertinent trends. One of the emphases of the review is compounds with biomedical potential.
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