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是一种半衰期为20.3分钟的短命放射性同位素，在生物化学研究、药物开发和诊断医学成像等方面有着重要的应用。由于碳原子构成了所有有机化合物和几乎所有生物分子、药物和显像剂的主干，碳-11是用途最广泛的同位素，用于制备这些标记的类似物用于成像，而不会改变它们在生命系统中的行为。为了合成碳-11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，以确保结果的重现性和产品的安全性和实用性。我们的研究项目用碳-11开发了改进的化学方法，并使用这种同位素开发了新的显像剂。具体地说，我们认为，将高氧化态碳-11标记与二氧化碳以及一氧化碳和氰化物等类似衍生物结合到分子中的方法将极大地扩大这种同位素的合成武器，并直接导致可用于分子成像的新型和改进的放射性药物。