|
|||||
|
|
Radiosynthesis of N-[11C]-methyl-hydroxyfasudil as a new potential PET radiotracer for rho-kinases (ROCKs) |
|
| Authors: | Ana C Valdivia Samantha Mason Jeffrey Collins Kenneth R Buckley Paul Coletta Rob S Beanlands Jean N DaSilva |
| Institution: | 1. School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China;2. International Joint Laboratory (SYSU-PolyU HK) of Novel Anti-dementia Drugs of Guangdong, Guangzhou 510006, China;3. National and Local United Engineering Lab of Drug ability and New Drugs Evaluation, Sun Yat-sen University, Guangzhou 510080, China;4. Department of TCM, the First Affiliated Hospital, Sun Yat-Sen University, Guangzhou 510080, China;5. Department of Applied Biology and Chemical Technology, Hong Kong Polytechnic University, Hong Kong, China;6. Guangdong Province Key Laboratory of Brain Function and Disease, Zhongshan School of Medicine, Sun Yat-sen University, Guangzhou 510080, China |
| Abstract: | N-11C]-methyl-hydroxyfasudil was synthesized as a new potential radiotracer for rho-kinases (ROCKs) via a two-step one-pot radiosynthesis. The first step was the methylation of the precursor N-Boc-hydroxyfasudil-sodium salt/benzo-15-crown-5 complex with 11C]methyl iodide. The second step involved deprotection of the tert-butoxycarbonyl protecting group. The radiochemical and chemical purities of N-11C]-methyl-hydroxyfasudil were >95% and specific radioactivity was 1565–2565 mCi/μmol at the end of the synthesis. |
| Keywords: | |
| 本文献已被 ScienceDirect 等数据库收录！ | |