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抑制中介的原氧化19F/18F-化阿里尔酸:一种机械指导的方法,用于优化PET探头开发
Jingkai Sun1, Carolin Jaworski2, Ralf Schirrmacher2
1Department of Chemistry, 4-010 CCIS, University of Alberta, Edmonton, Alberta, T6G 2G2, Canada.
Chemistry (Weinheim an der Bergstrasse, Germany)
|July 3, 2024
概括
这项研究提出了一种新的,高效的铜介导法,用于化甲酸和. 改进的协议最大限度地减少了proto-deboronation,提高了药物发现和医学成像应用的产量.
科学领域:
- 有机化学 有机化学
- 药用化学 医学化学
- 放射化学 放射化学是指辐射化学.
背景情况:
- 化在制药,材料科学和医学成像中至关重要.
- 现有的以铜为媒介的化法对甲酸经常遭受原甲酸,复杂的净化和放射性追踪器的有效性.
- 需要更简单,更有效的化协议来最大限度地减少原化.
研究的目的:
- 开发一种快速高效的18F/19F化法,用于化酸和 Ester.
- 为了尽量减少铜介导化过程中的原氧化.
- 建立一个适用于一般化烯合成和18F放射性化两种方法的协议.
主要方法:
- 机械学研究确定了高温和强的供体配体 (乙二,二) 作为原体激发的促进剂.
- 优化导致了一种使用t-BuOH作为溶剂的无链体程序,在较温和的条件下激活化物.
- 为了提高化效率,使用了一种新型的铜盐Cu ((ONf) 2).
主要成果:
- 优化的无结合体,温和温度协议可以最大限度地减少proto-deboronation.
- 该程序可以容忍广泛的功能组,在60°C时在30分钟内完成.
- 化和异的产量在39%至84%之间.
- 适应18F放射性化实现了17-54%的放射性化学转换,并显著减少了原化.
结论:
- 已经建立了一种新的,高效的,更温和的铜介导化协议,用于甲酸和 Ester.
- 这种方法有效地抑制了原化,提高了产量和在放射性追踪器开发中的适用性.
- 该协议为合成化化合物提供了一种有价值的工具,用于各种应用,包括体内成像.
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