Publication details for Prof. Graham SandfordWillis, N.J., Fisher, C.A., Alder, C.M., Harsanyi, A., Shukla, L., Adams, J.P. & Sandford, G. (2016). Sustainable synthesis of enantiopure fluorolactam derivatives by a selective direct fluorination – amidase strategy. Green Chemistry 18(5): 1313-1318.
- Publication type: Journal Article
- ISSN/ISBN: 1463-9262, 1463-9270
- DOI: 10.1039/C5GC02209F
- Further publication details on publisher web site
- Durham Research Online (DRO) - may include full text
Author(s) from Durham
Pharmaceutically important chiral fluorolactam derivatives bearing a fluorine atom at a stereogenic centre were synthesized by a route involving copper catalyzed selective direct fluorination using fluorine gas for the construction of the key C–F bond and a biochemical amidase process for the crucial asymmetric cyclisation stage. A comparison of process green metrics with reported palladium catalyzed enantioselective fluorination methodology shows the fluorination-amidase route to be very efficient and more suitable for scale-up.