Långström B, Antoni G, Bjurling P, Fasth K J, Gee A D, Någren K, Ulin J
Department of Organic Chemistry, University of Uppsala, Sweden.
Acta Radiol Suppl. 1990;374:147-51.
The future impact of positron emission tomography in clinical and basic sciences will be closely related to further developments of detector systems with regard to sensitivity and resolution, but probably even more with respect to developments in the synthesis of relevant labeled tracer molecules. Among the interesting radionuclides, 11C is of special interest since it is a radionuclide of an element, carbon, frequently occurring in the biosystem. In this paper some of the recent progress within the field of using the short-lived radionuclide 11C with a half-life of 20.4 min is presented. The paper deals with synthetic strategies which have been applied starting from simple one-carbon precursors like 11C carbon dioxide. In these strategies the development of reliable methods for production of one-carbon and multiple-carbon precursors, as well as multiple-carbon difunctional precursors, is important. Some examples are discussed. Labeled precursors can be applied conventional types of organic synthesis, in enzyme catalyzed reactions, or by using a combination of these. The synthesis of interesting 11C labeled receptor ligands and amino acids such as alanine, valine, phenylalanine, DOPA, tryptophan, 5-hydroxytryptophan, 2-methyltyrosine and some neuropeptides are presented.
正电子发射断层扫描在临床和基础科学领域的未来影响将与探测器系统在灵敏度和分辨率方面的进一步发展密切相关,但可能更与相关标记示踪分子合成方面的发展有关。在众多有趣的放射性核素中,11C 特别引人关注,因为它是碳元素的一种放射性核素,而碳在生物系统中经常出现。本文介绍了近期在使用半衰期为 20.4 分钟的短寿命放射性核素 11C 领域取得的一些进展。本文探讨了从诸如 11C 二氧化碳等简单的一碳前体开始应用的合成策略。在这些策略中,开发可靠的生产一碳和多碳前体以及多碳双官能前体的方法很重要。文中讨论了一些实例。标记前体可应用于传统类型的有机合成、酶催化反应或两者结合的反应。文中介绍了有趣的 11C 标记受体配体和氨基酸的合成,如丙氨酸、缬氨酸、苯丙氨酸、多巴、色氨酸、5-羟色氨酸、2-甲基酪氨酸以及一些神经肽。