Synthesis of an 11C-Labeled Antiprion GN8 Derivative and Evaluation of Its Brain Uptake by Positron Emission Tomography

Synthesis of an 11C-Labeled Antiprion GN8 Derivative and Evaluation of Its Brain Uptake by Positron Emission Tomography
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11C 标记的 Antiprion GN8 衍生物的合成及其脑摄取的正电子发射断层扫描评估

DOI:
10.1002/cmdc.201300167
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发表时间:
2013
期刊:
影响因子:
3.4
通讯作者:
Kazuo Kuwata
Kazuo Kuwata
中科院分区:
医学4区
文献类型:
--
作者:
Tsutomu Kimura;Takeo Sako;Siqin;Junji Hosokawa-Muto;Yi Long Cui;Yasuhiro Wada;Yosky Kataoka;Hisashi Doi;Suehiro Sakaguchi;Masaaki Suzuki;Yasuyoshi Watanabe;Kazuo Kuwata

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一个放射性标记的PET!用钯催化的芳基三丁基锡烷快速甲基化反应合成了一种抗朊病毒药物N,N ′-(亚甲基二-4,1-亚苯基)二[2-(1-吡咯烷基)乙酰胺](GN 8)的(11)C-标记衍生物,并用正电子发射断层扫描(PET)评价了其在大鼠体内的脑渗透和器官分布。
A radiolabeled PET! A (11) C-labeled derivative of N, N'-(methylenedi-4, 1-phenylene) bis [2-(1-pyrrolidinyl) acetamide](GN8), an antiprion agent currently under development, was synthesized by palladium-catalyzed rapid methylation of aryltributylstannane and assessed for brain penetration and organ distribution in rats by positron emission tomography (PET).