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.