Innovative trifluoromethyls using boronic building blocks
Newsletter N° 20 - February 2012
Trifluoromethylated molecules are increasingly used in the pharma and crop protection industries, thanks to their positive influence on the biological properties of active compounds.1
Trifluoromethyl containing active pharma and agrochemical products
The availability of synthetic methods enabling the trifluoromethylation of either aromatics or heteroaromatics in medicinal chemistry is of high importance. Electrophilic trifluoromethylation, however, requires harsh conditions and the traditional synthetic methods have earned a reputation as being difficult to achieve.2
New methods have recently been discovered to obtain trifluoromethylated heterocycles under mild conditions.3, 4, 5
Copper-catalyzed trifluoromethylation of boronic acids
The latest trifluoromethylation methods use boronic compounds to achieve fluorinated compounds. The great variety of boronic building blocks commercially available today offers great potential for developing a large array of fluorinated compounds.
Trifluoromethylation applied to a sample of borochem catalogue compounds
Trifluoromethylation can be applied to a wide range of compounds.
Search our online database of boronic compounds to facilitate your inhouse synthesis of trifluoromethylated heterocycles, or call on BoroChem's chemistry team for tailor-made new compounds.
1. Chem. Soc. Rev., 2008, 37, 320
2. Organofluorine Chemistry, 2006, K. Uneyama
3. Org. Lett, 2010, 12 (21), 5060
4. Chem. Commun., 2011, 47, 4300
5. J. Org. Chem., 2011, 76 (17), 1174