June 2, 2016
Developing pharmaceuticals and agrochemicals using inexpensive and readily available acid anhydride
Perfluoroalkyl compounds with CnH2n+1 hydrogen atoms substituted with fluorine are attractive as drug candidates, as they are known to have improved lipophilicity and metabolic stability. A number of research groups in Japan and internationally have been actively working on synthetic methods for perfluoroalkyl compounds, but most of the currently reported methods are not ideal for industrial application due to the usage of expensive reagents and safety issues.
RIKEN CSRS researchers used trifluoromethyl anhydride and other perfluoro anhydrides to perfluoroalkylate alkenes to efficiently and conveniently synthesize trifluoromethyl and other perfluoroalkyl compounds. This very practical method uses inexpensive and readily available perfluoro acid anhydride. Since the obtained perfluoro group–bearing products are useful as “building blocks,” this new method will facilitate the development of pharmaceuticals and agrochemicals.
Angewandte Chemie International Edition doi:10.1002/anie.201604127
S. Kawamura, M. Sodeoka,
"Perfluoroalkylation of Unactivated Alkenes with Acid Anhydrides as the Perfluoroalkyl Source".
Mikiko Sodeoka; Group Director
Shintaro Kawamura; Postdoctoral Researcher
Catalysis and Integrated Research Group