Herein, we present a fast, efficient and general one-pot method for the synthesis of ¹¹C-labelled compounds via the Negishi cross-coupling reaction. Our approach, based on the in situ formation of [¹¹C]CH₃ZnI and subsequent reaction with aryl halides or triflates, has proven efficient to synthesize [¹¹C]thymidine, a biologically relevant compound with potential applications as a proliferation marker. Theoretical calculations have shown irreversible formation of a tetracoordinated nucleophilic ¹¹C–Zn(II) reagent and electronic requirements for an efficient Negishi coupling.

中文翻译：

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Negishi与[ ¹¹ C] CH ₃ I的偶联反应：有效形成¹¹ C–C键的通用方法†

在这里，我们提出了一种通过Negishi交叉偶联反应合成¹¹ C标记化合物的快速，有效和通用的一锅法。我们的方法基于[ ¹¹ C] CH ₃ ZnI的原位形成并随后与芳基卤化物或三氟甲磺酸酯反应，已被证明可有效地合成[ ¹¹ C]胸苷，这是一种生物学相关的化合物，具有潜在的增殖标记作用。理论计算表明，四配位亲核¹¹ C-Zn（II）试剂的不可逆形成和有效Negishi偶联的电子要求。