Radiosynthesis of N-[(11)C]-methyl-hydroxyfasudil as a new potential PET radiotracer for rho-kinases (ROCKs).

作者信息

Valdivia Ana C, Mason Samantha, Collins Jeffrey, Buckley Kenneth R, Coletta Paul, Beanlands Rob S, Dasilva Jean N

机构信息

National Cardiac PET Centre, University of Ottawa Heart Institute, 40 Ruskin Street, Ottawa, Ont., Canada K1Y 4W7.

出版信息

Appl Radiat Isot. 2010 Feb;68(2):325-8. doi: 10.1016/j.apradiso.2009.11.002. Epub 2009 Nov 10.

N-[(11)C]-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 [(11)C]methyl iodide. The second step involved deprotection of the tert-butoxycarbonyl protecting group. The radiochemical and chemical purities of N-[(11)C]-methyl-hydroxyfasudil were >95% and specific radioactivity was 1565-2565mCi/mumol at the end of the synthesis.