Trifluoromethylation of Highly Functionalized Heteroarenes: Flow to the Rescue

Timothy Nöel and Jesus Alcazar describe the trifluoromethylation of highly functionalized heteroarenes.

Visible-Light-Induced Trifluoromethylation of Highly Functionalized Arenes and Heteroarenes in Continuous Flow: I. Abdiaj, C. Bottecchia, J. Alcazar, T. Noёl Synthesis 2017, DOI: 10.1055/s-0036-1588527

The trifluoromethyl group is not present in nature but is widely present in synthetic drugs and bioactive compounds. For this reason, methods for incorporating this man-made, xenobiotic function into organic molecules continue to attract the interest of organic and medicinal chemists. The group of Professor Timothy Nöel, from the Eindhoven University of Technology (The Netherlands), in collaboration with the pharmaceutical company Janssen (Toledo, Spain), recently reported a new trifluoromethylation strategy induced by visible light and performed in conditions of continuous flow.

Professor Nöel said: “In our interest to develop a broadly applicable trifluoromethylation strategy for highly functionalized heteroarenes we envisioned a practical continuous flow procedure affording the desired trifluoromethylated derivatives within only 30 minutes of residence time. Owing to the improved safety of operation and the reliable scale-up, continuous flow reactors are ideal candidates to accelerate drug discovering processes.”