Fluorine shows up only rarely in naturally-occurring compounds, so biocatalysis offers few realistic options. Yet, for drugs and plant protection agents, about 25% of compounds in development contain fluorine.
Why? Because fluorine-containing functionality often improves bioavailability and metabolic stability. For this reason, finding practical ways to introduce fluorine is attracting a lot of attention form chemists. Trifluoromethylation is even more difficult than fluorination.
A new company named Catylix, Inc. co-founded by Professor John Hartwig (previously at the University of Illinois where the technology was developed and patented; now at UC Berkeley) and Dr. David Rozzell (that’s me) is offering a new method for trifluoromethylation with unprecedented scope and functional group compatibility. The first product, a shelf-stable reagent for trifluoromethylation of aryl and vinyl iodides and bromides, was launched in July 2011 and is available through Aldrich.
The main targeted applications are late-stage trifluoromethylation for lead compound by medicinal chemists and the development of new plant protection agents, but wider applications are envisioned in the future.
For more information on the trifluoromethylation chemistry and new shelf-stable reagent, please check out the Catylix web site