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

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 involve...

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Veröffentlicht in:	Applied radiation and isotopes 2010-02, Vol.68 (2), p.325-328
Hauptverfasser:	Valdivia, Ana C., Mason, Samantha, Collins, Jeffrey, Buckley, Kenneth R., Coletta, Paul, Beanlands, Rob S., DaSilva, Jean N.
Format:	Artikel
Sprache:	eng
Schlagworte:	1-(5-Isoquinolinesulfonyl)-2-Methylpiperazine - analogs & derivatives 1-(5-Isoquinolinesulfonyl)-2-Methylpiperazine - chemistry 1-(5-Isoquinolinesulfonyl)-2-Methylpiperazine - pharmacokinetics Carbon-11 Fasudil Feasibility Studies Hydroxyfasudil Image Enhancement - methods Intracellular labeling Isotope Labeling - methods Positron-Emission Tomography - methods Radiopharmaceuticals - chemical synthesis Radiopharmaceuticals - pharmacokinetics rho-Associated Kinases - metabolism Rho-kinases
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Zusammenfassung:	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.
ISSN:	0969-8043 1872-9800
DOI:	10.1016/j.apradiso.2009.11.002