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99mTc 为中心的一锅合成法用于制备 99mTc 放射性示踪剂。

99mTc-centered one-pot synthesis for preparation of 99mTc radiotracers.

机构信息

School of Health Sciences, Purdue University 550 Stadium Mall Drive, West Lafayette, IN 47907, USA.

出版信息

Dalton Trans. 2011 Jun 21;40(23):6077-86. doi: 10.1039/c0dt01462a. Epub 2011 Mar 3.

DOI:10.1039/c0dt01462a
PMID:21373664
Abstract

Nuclear medicine relies on two main imaging modalities: single photon emission computed tomography (SPECT) and positron emission tomography (PET). Radiopharmaceuticals (or radiotracers) are the blood stream of nuclear medicine for the diagnosis or therapy of diseases. Diagnostic radiotracers that are small molecules labelled with a gamma-emitter for SPECT or positron-emitter for PET provide a non-invasive method to assess the disease or disease states and monitor the therapeutic efficacy of a specific treatment regime. Over the past four decades, radiopharmaceutical research has been practising one-pot synthesis at the tracer level (10(-7)-10(-6) M). Many (99m)Tc radiotracers currently used in nuclear medicine are routinely prepared by following the basic principles of one-pot synthesis. Unlike traditional organic one-pot synthesis, which often involves the formation of multiple C-C and C-heteroatom bonds in a single step, the (99m)Tc-centered one-pot synthesis requires the formation of multiple coordination bonds between Tc and various donor atoms, such as N, O, S and P. This review will illustrate how the (99m)Tc-centered one-pot synthesis is utilized for routine preparations of different (99m)Tc radiotracers.

摘要

核医学依赖于两种主要的成像方式

单光子发射计算机断层扫描(SPECT)和正电子发射断层扫描(PET)。放射性药物(或放射性示踪剂)是核医学的血流,用于疾病的诊断或治疗。用伽马发射器标记的小分子作为 SPECT 的诊断放射性示踪剂或正电子发射器用于 PET 的放射性示踪剂提供了一种非侵入性的方法来评估疾病或疾病状态,并监测特定治疗方案的治疗效果。在过去的四十年中,放射性药物研究一直在示踪剂水平(10(-7)-10(-6) M)进行一锅合成实践。目前在核医学中使用的许多 (99m)Tc 放射性示踪剂都是按照一锅合成的基本原理常规制备的。与传统的有机一锅合成不同,后者通常涉及在单个步骤中形成多个 C-C 和 C-杂原子键,(99m)Tc 为中心的一锅合成需要在 Tc 和各种供体原子(如 N、O、S 和 P)之间形成多个配位键。这篇综述将说明如何利用 (99m)Tc 为中心的一锅合成常规制备不同的 (99m)Tc 放射性示踪剂。

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