From [11C]CO2 to [11C] amides: a rapid one-pot synthesis via the Mitsunobu reaction
From [11C]CO2 to [11C] amides: a rapid one-pot synthesis via the Mitsunobu reaction
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DOI：
10.1039/c7cc01407d
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发表时间：
2017-05-11
影响因子：
4.9
通讯作者：
Gee, A. D.
中科院分区：
文献类型：
--
作者：
Bongarzone, S.;Runser, A.;Gee, A. D.
介绍了一种利用胺、CO2、格氏试剂和光信试剂合成酰胺的新方法。该方法应用于碳-11放射化学，利用回旋加速器产生的[C-11] CO2标记酰胺。通过生产[C-11]褪黑激素，证明了一罐标记方法的合成效用。用放射高效液相色谱法测定[C-11] CO2在[C-11] CO2递送后2分钟内与[C-11]褪黑素的掺入率为36%。
A novel amide synthesis methodology is described using amines, CO2] and Grignard reagents and Mitsunobu reagents. The method was applied to carbon-11 radiochemistry to label amides using cyclotron-produced [C-11] CO2. The synthetic utility of the one-pot labellingmethodology was demonstrated by producing [C-11] melatonin. The incorporation of [C-11] CO2 into [C-11] melatonin was 36% determined by radioHPLC 2 min post [C-11] CO2 delivery.