Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10588838 | Bioorganic & Medicinal Chemistry Letters | 2010 | 4 Pages |
Abstract
Radiosynthesis and in vivo evaluation of [N-methyl-11C] 5-methyl-3-[4-(3-phenylallyl)-piperazin-1-ylmethyl]-3,3a,4,5-tetrahydroisoxazolo[4,3-c]quinoline (1), a potential PET tracer for alpha2-adrenergic receptors is described. Syntheses of nonradioactive standard 1 and corresponding desmethyl precursor 2 were achieved from 2-aminobenzaldehyde in 40% and 65% yields, respectively. Methylation using [11C]CH3I in presence of aqueous potassium hydroxide in DMSO afforded [11C]1 in 25% yield (EOS) with >99% chemical and radiochemical purities with a specific activity ranged from 3-4 Ci/μmol (n = 6). The total synthesis time was 30 min from EOB. PET studies in anesthetized baboon show that [11C]1 penetrates BBB and accumulates in alpha2A-AR enriched brain areas.
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Authors
Jaya Prabhakaran, Vattoly J. Majo, Matthew S. Milak, Pratap Mali, Lyudmila Savenkova, J. John Mann, Ramin V. Parsey, J.S. Dileep Kumar,