Synthesis of new carbon-11-labeled carboxamide derivatives as potential PET dopamine D3 receptor radioligands
Synthesis of new carbon-11-labeled carboxamide derivatives as potential PET dopamine D3 receptor radioligands
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DOI：
10.1016/j.apradiso.2008.05.010
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发表时间：
2008-12-01
影响因子：
1.6
通讯作者：
Zheng, Qi-Huang
中科院分区：
文献类型：
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作者：
Gao, Mingzhang;Wang, Min;Zheng, Qi-Huang
碳-11标记的羧胺衍生物，(E)-4-fluoro-N-(4-(4-(2-[(11)Clmethoxyphenyl)piperazin-1-yl)butyl)cinnamoylamide，([C-11]3a)，(E)-4-chloro-N-(4-(4-(2-[(11)Cimethoxyphenyl)piperazin-1-yl)butyl)肉桂酰胺([C-11]3b)，(E)-4-bromo-N-(4-(4-(2-[C-11]methoxyphenyl)piperazin-1-yl)butyl)cinnamoylamide，([C-11]3c)、(E)-4-methoxy-N-(4-(4-(2-[C-11]methoxyphenyl)piperazin-1-yl)butyl)cinnamoylamide([C-11]3D)、N-(4-(4-(2-[C-11]methoxyphenyl)piperazin-1-yl)butyl)naphthyl-2-carboxamide([C-11]BP897、[C-11]3e)和N-(4-(4-(2-[C-11]methoxyphenyl)piperazin-1-yl)butyl)biphenyl-4-carboxamide([C-11]3f)作为新的多巴胺D-3受体显像剂。目标示踪剂是用[C-11]CH3OTf对其相应的前体进行O-[C-11]甲基化制备的，并通过简化的固相萃取(SPE)纯化程序进行分离，放化产率为50-65%，衰变校正到轰击结束(EOB)，总合成时间为20min，合成结束时的比活度(EOS)为111-148GBq/u。(C)2008爱思唯尔有限公司。保留所有权利
Carbon-11-labeled carboxamide derivatives, (E)-4-fluoro-N-(4-(4-(2-[(11)Clmethoxyphenyl)piperazin-1-yl)butyl)cinnamoylamide, ([C-11]3a), (E)-4-chloro-N-(4-(4-(2-[(11)Cimethoxyphenyl)piperazin-1-yl)butyl) cinnamoylamide ([C-11]3b), (E)-4-bromo-N-(4-(4-(2-[C-11]methoxyphenyl)piperazin-1-yl)butyl)cinnamoylamide, ([C-11]3c), (E)-4-methoxy-N-(4-(4-(2-[C-11]methoxyphenyl)piperazin-1-yl)butyl)cinnamoylamide ([C-11]3d), N-(4-(4-(2-[C-11]methoxyphenyl)piperazin-1-yl)butyl)naphthyl-2-carboxamide ([C-11]BP897, [C-11]3e), and N-(4-(4-(2-[C-11]methoxyphenyl)piperazin-1-yl)butyl)biphenyl-4-carboxamide ([C-11]3f), have been synthesized as new potential PET radioligands for imaging of dopamine D-3 receptors. The target tracers were prepared by O-[C-11]methylation of their corresponding precursors using [C-11]CH3OTf and isolated by a simplified solid-phase extraction (SPE) purification procedure in 50-65% radiochemical yields decay corrected to end of bombardment (EOB), 20 min overall synthesis time, and 111-148GBq/mu mol specific activity at end of synthesis (EOS). (C) 2008 Elsevier Ltd. All rights reserved