Radiosynthesis of N-[(11)C]-methyl-hydroxyfasudil as a new potential PET radiotracer for rho-kinases (ROCKs).
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.
Valdivia
Ana C
AC
National Cardiac PET Centre, University of Ottawa Heart Institute, 40 Ruskin Street, Ottawa, Ont., Canada K1Y 4W7.
Mason
Samantha
S
Collins
Jeffrey
J
Buckley
Kenneth R
KR
Coletta
Paul
P
Beanlands
Rob S
RS
Dasilva
Jean N
JN
D019307:1-(5-Isoquinolinesulfonyl)-2-Methylpiperazine / Q000031:analogs & derivatives* / Q000737:chemistry / Q000493:pharmacokinetics; D005240:Feasibility Studies; D007089:Image Enhancement / Q000379:methods; D007553:Isotope Labeling / Q000379:methods; D049268:Positron-Emission Tomography / Q000379:methods*; D019275:Radiopharmaceuticals / Q000138:chemical synthesis / Q000493:pharmacokinetics; D054460:rho-Associated Kinases / Q000378:metabolism*
C547762:N-methyl-hydroxyfasudil; D019275:Radiopharmaceuticals; D019307:1-(5-Isoquinolinesulfonyl)-2-Methylpiperazine; D054460:rho-Associated Kinases