|
|||||
|
|
[F]Fluoroamines via ring-opening of N-Cbz-2-methylaziridine with [F]-fluoride |
|
| Authors: | Neil Vasdev Erik M. van Oosten Karin A. Stephenson Nonik Zadikian Andrei K. Yudin Sylvain Houle Alan A. Wilson |
| Affiliation: | a Centre for Addiction and Mental Health, 250 College St., Toronto, Ontario, Canada M5T 1R8 b Department of Psychiatry, University of Toronto, 250 College St., Toronto, Ontario, Canada M5T 1R8 c Department of Chemistry, University of Toronto, 80 St. George St., Toronto, Ontario, Canada M5S 3H6 |
| Abstract: | A highly regioselective method was developed for ring-opening benzyloxycarbonyl (Cbz)-protected 2-methylaziridine with [18F]-labelled fluoride. Following catalytic hydrogenation, 1-[18F]fluoro-2-propanamine ([18F]1) and 2-[18F]fluoro-1-propanamine ([18F]2) were prepared as the major and minor products, respectively (85:15), and were characterized following acylation with benzyl chloride. This methodology is applicable towards the generation of new [18F]-labelled amines for incorporation into radiopharmaceuticals. |
| Keywords: | Aziridine Fluorine-18 Ring-opening Fluoroisopropylamine PET 1-Fluoro-2-propanamine 2-Fluoro-1-propanamine |
| 本文献已被 ScienceDirect 等数据库收录！ | |