Synthesis of 2-trifluoromethylated piperidines and azepanes by Sarah Rioton

The incorporation of fluorine atom in organic compounds can have a profound impact on the physico-chemical properties and, therefore, on the biological activity of the molecules. Thus, amines possessing an α-trifluoromethyl substituent are of great importance in medicinal chemistry, as amines are present in a variety of bioactive compounds.

During researches which led to a new synthetic route of enantioenriched 3‑substituted 2-(trifluoromethyl)piperidines and 4‑substituted 2‑(trifluoromethyl)azepanes by stereospecific ring expansion of trifluoromethylated pyrrolidines, the state of the art regarding the others synthetic methods of these products was examined and is shared in this collection.