New approaches to carbon-11 labeled carbonyl and thiocarbonyl groups for positron emission tomography radiotracer synthesis and development

用于正电子发射断层扫描放射性示踪剂合成和开发的碳 11 标记羰基和硫代羰基的新方法

• 批准号: RGPIN-2017-06167
• 负责人: Rotstein, Benjamin
• 金额: $ 2.4万
• 依托单位: University of Ottawa
• 依托单位国家: 加拿大
• 项目类别: Discovery Grants Program - Individual
• 财政年份: 2017
• 资助国家: 加拿大
• 起止时间: 2017-01-01 至 2018-12-31
• 项目状态: 已结题
• 来源: https://www.nserc-crsng.gc.ca/ase-oro/Details-Detailles_eng.asp?id=632658
• 关键词: New; approaches; carbon; 11; labeled

Carbon-11 is a short-lived radioactive isotope with a half-life of 20.3 minutes, and which has important applications for biochemistry research, drug development, and diagnostic medical imaging. Since carbon atoms form the backbone of all organic compounds and nearly all biomolecules, drugs, and imaging agents, carbon-11 is the most versatile isotope for preparing labeled analogues of these for imaging without changing their behaviour in living systems. To synthesize imaging agents with carbon-11, chemical transformations need to be performed in rapid succession with high efficiency under strictly controlled conditions to ensure reproducible results and the safety and utility of products. Our research program develops improved chemical methods with carbon-11 and new imaging agents using this isotope. Specifically, we believe that methods for incorporating high oxidation state carbon-11 labels into molecules from its production form as carbon dioxide and similar derivatives such as carbon monoxide and cyanide will greatly expand the synthetic armament for this isotope and directly lead to novel and improved radiopharmaceuticals available to power molecular imaging.

碳11是一种短寿命放射性同位素，半衰期为20.3分钟，在生物化学研究、药物开发和诊断医学成像方面具有重要应用。由于碳原子构成所有有机化合物以及几乎所有生物分子、药物和成像剂的主链，因此碳 11 是最通用的同位素，可用于制备这些标记类似物以进行成像，而无需改变它们在生命系统中的行为。为了用碳11合成显像剂，需要在严格控制的条件下快速、连续、高效地进行化学转化，以确保结果的可重复性以及产品的安全性和实用性。我们的研究项目开发了改进的碳 11 化学方法以及使用该同位素的新型显像剂。具体来说，我们相信，将高氧化态碳 11 标记结合到二氧化碳和类似衍生物（例如一氧化碳和氰化物）的分子中的方法将极大地扩展该同位素的合成武器，并直接导致新型和改进的放射性药物可用于驱动分子成像。