Strategies for the Production of [11C]LY2795050 for Clinical Use.
Strategies for the Production of [11C]LY2795050 for Clinical Use.
复制标题
临床用[11C]LY2795050 的生产策略。
DOI：
10.1021/acs.oprd.2c00388
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发表时间：
2023
影响因子：
3.4
通讯作者：
Scott,PeterJH
中科院分区：
文献类型：
--
作者：
Kaur,Tanpreet;Shao,Xia;Horikawa,Mami;Sharninghausen,LiamS;Preshlock,Sean;Brooks,AllenF;Henderson,BradfordD;Koeppe,RobertA;DaSilva,AlexandreF;Sanford,MelanieS;Scott,PeterJH
这份报告描述了四种不同的κ-阿片受体拮抗剂[11C]LY2795050临床规模放射合成的比较。研究了钯催化的芳基碘化物前驱体的放射性氰化反应和放射性羰基化反应，以及铜催化的芳基碘化合物和芳基硼酸酯的放射氰化反应。报告了所有四种方法的全自动化，每一种方法都提供了[11C]LY2795050，具有足够的放射化学产率、摩尔活度和放射化学纯度，供临床使用。比较和对比了各种放射合成方法的优缺点。
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.