This report describes a comparison of four different routes for the clinical-scale radiosynthesis of the κ-opioid receptor antagonist [¹¹C]LY2795050. Palladium-mediated radiocyanation and radiocarbonylation of an aryl iodide precursor, as well as copper-mediated radiocyanation of an aryl iodide and an aryl boronate ester, have been investigated. Full automation of all four methods is reported, each of which provides [¹¹C]LY2795050 in sufficient radiochemical yield, molar activity, and radiochemical purity for clinical use. The advantages and disadvantages of each radiosynthesis method are compared and contrasted.

中文翻译：

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临床用 [11C]LY2795050 的生产策略

本报告描述了 κ-阿片受体拮抗剂 [ ¹¹ C]LY2795050 临床规模放射合成的四种不同途径的比较。已经研究了钯介导的芳基碘化物前体的放射性氰化和放射性羰基化，以及铜介导的芳基碘化物和芳基硼​​酸酯的放射性氰化。报告了所有四种方法的完全自动化，每种方法都提供了足够的 [ ¹¹ C]LY2795050 放射化学产率、摩尔活性和放射化学纯度供临床使用。对每种放射合成方法的优缺点进行了比较和对比。