临床用[11C]LY2795050的生产策略

IF 3.5 3区化学 Q2 CHEMISTRY, APPLIED

Organic Process Research & Development Pub Date : 2023-02-08 DOI:10.1021/acs.oprd.2c00388

Tanpreet Kaur, Xia Shao, Mami Horikawa, Liam S. Sharninghausen, Sean Preshlock, Allen F. Brooks, Bradford D. Henderson, Robert A. Koeppe, Alexandre F. DaSilva, Melanie S. Sanford* and Peter J. H. Scott*,

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引用次数: 2

摘要

本报告比较了4种不同途径的κ-阿片受体拮抗剂[11C]LY2795050的临床放射合成。钯介导的放射性氰化和碘化芳基前体的放射性羰基化，以及铜介导的碘化芳基和硼酸芳基酯的放射性氰化，已经进行了研究。据报道，所有四种方法的完全自动化，每种方法都为临床提供了足够的放射化学产率，摩尔活性和放射化学纯度[11C]LY2795050。对各种放射性合成方法的优缺点进行了比较和对比。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

Strategies for the Production of [11C]LY2795050 for Clinical Use

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Strategies for the Production of [11C]LY2795050 for Clinical Use

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.

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来源期刊

Organic Process Research & Development 化学-应用化学

CiteScore

6.90

自引率

14.70%

发文量

251

审稿时长

2 months

期刊介绍： The journal Organic Process Research & Development serves as a communication tool between industrial chemists and chemists working in universities and research institutes. As such, it reports original work from the broad field of industrial process chemistry but also presents academic results that are relevant, or potentially relevant, to industrial applications. Process chemistry is the science that enables the safe, environmentally benign and ultimately economical manufacturing of organic compounds that are required in larger amounts to help address the needs of society. Consequently, the Journal encompasses every aspect of organic chemistry, including all aspects of catalysis, synthetic methodology development and synthetic strategy exploration, but also includes aspects from analytical and solid-state chemistry and chemical engineering, such as work-up tools，process safety, or flow-chemistry. The goal of development and optimization of chemical reactions and processes is their transfer to a larger scale; original work describing such studies and the actual implementation on scale is highly relevant to the journal. However, studies on new developments from either industry, research institutes or academia that have not yet been demonstrated on scale, but where an industrial utility can be expected and where the study has addressed important prerequisites for a scale-up and has given confidence into the reliability and practicality of the chemistry, also serve the mission of OPR&D as a communication tool between the different contributors to the field.