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- W2065293670 abstract "To develop novel short-lived 11C radionuclide-incorporated PET tracers with high metabolic tolerance, we performed rapid methylation using 11CH3I, a frequently used precursor for 11C-labeled tracers, on sp- and sp2-carbon frameworks. Methyl iodide was trapped using an excess of tributylphenylstannane for 5 min at 60 °C in the presence of Pd[P(o-tolyl)3]2, a copper(I) salt (CuCl or CuBr), and K2CO3, resulting in a greater than 90% yield of toluene. A trapping reaction with tributyl-1-hexynylstannane for 5 min at 60 °C in the presence of Pd[P(t-C4H9)3]2 and a fluoride ion (KF or CsF) gave a high yield (>90%) of 2-heptyne. Since these reactions are applicable to a wide range of organic molecules, we synthesized 15R-[11C]TIC methyl ester, a PET tracer targeting the CNS-specific prostacyclin receptor (IP2), by rapid sp2–sp3 coupling with some modifications. Radiolabeled 11CH3I was trapped with the methyl ester of the corresponding stannyl precursor via two steps. In the first, 11CH3I and Pd[P(o-tolyl)3]2 were mixed to form a methylpalladium complex, and in the second, the methylpalladium complex was mixed with the other reagents necessary for the coupling reaction. The yield of radiolabeled 15R-[11C]TIC methyl ester was 80–90%, and it had a radioactivity of 2.0–2.5 GBq, sufficient for an in vivo human PET study with high reproducibility. We used this tracer in PET studies imaging the IP2 receptor in living monkey and human brains. Following its penetration of the blood–brain barrier, the tracer underwent ester hydrolysis and bound to its specific receptor in the brain. A protocol for sp–sp3 coupling would be used to synthesize [11C]iloprost methyl ester, a PET tracer for the peripheral-type prostacyclin receptor (IP1). A methyl group is the least bulky, unpolarized organic group, suggesting that it would have little effect on the biological activity of its parent compound. Thus, [11C]methylated compounds may be applicable to a wide range of biologically active molecules, converting them to PET tracers that can be utilized for in vivo molecular imaging." @default.
- W2065293670 created "2016-06-24" @default.
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- W2065293670 date "2004-09-01" @default.
- W2065293670 modified "2023-10-16" @default.
- W2065293670 title "Rapid methylation on carbon frameworks leading to the synthesis of a PET tracer capable of imaging a novel CNS-type prostacyclin receptor in living human brain" @default.
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- W2065293670 doi "https://doi.org/10.1016/j.trac.2004.06.003" @default.
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