Direct Carbon Isotope Exchange through Decarboxylative Carboxylation
Direct Carbon Isotope Exchange through Decarboxylative Carboxylation
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DOI：
10.1021/jacs.8b12035
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发表时间：
2019-01-16
影响因子：
15
通讯作者：
Baran, Phil S.
中科院分区：
文献类型：
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作者：
Kingston, Cian;Wallace, Michael A.;Baran, Phil S.
提出了烷基羧酸~(14)C标记的两步降解重建方法。通过氧化还原活性酯的形成进行简单的活化，然后镍介导的脱羧化得到一系列具有丰富的同位素结合的复杂化合物，用于药物代谢和药代动力学研究。该协议的实用性和操作简单性通过在工业碳14标记环境中的使用得到了证明。
A two-step degradation reconstruction approach to the carbon-14 radiolabeling of alkyl carboxylic acids is presented. Simple activation via redox-active ester formation was followed by nickel mediated decarboxylative carboxylation to afford a range of complex compounds with ample isotopic incorporations for drug metabolism and pharmacokinetic studies. The practicality and operational simplicity of the protocol were demonstrated by its use in an industrial carbon-14 radiolabeling setting.