药物与标记 CO 的动态碳同位素交换
Dynamic Carbon Isotope Exchange of Pharmaceuticals with Labeled CO.
机构信息
Service de Chimie Bio-organique et Marquage (SCBM), CEA/DRF/JOLIOT, Université Paris Saclay , F-91191 Gif-sur-Yvette , France.
NIMBE, CEA, CNRS, Université Paris-Saclay , F-91191 Gif-sur-Yvette , France.
出版信息
J Am Chem Soc. 2019 Jan 16;141(2):780-784. doi: 10.1021/jacs.8b12140. Epub 2018 Dec 31.
A copper-catalyzed procedure enabling dynamic carbon isotope exchange is described. Utilizing the universal precursor [C]CO, this protocol allows to insert, in one single step, the desired carbon tag into carboxylic acids with no need of structural modifications. Reducing synthetic costs and limiting the generation of radioactive waste, this procedure will facilitate the access to carboxylic acids containing drugs and accelerate early C-based ADME studies supporting drug development.
本文描述了一种铜催化的动态碳同位素交换方法。利用通用前体[C]CO，该方案可以一步将所需的碳标记插入到羧酸中，而无需进行结构修饰。这种方法降低了合成成本，限制了放射性废物的产生，将有助于获得含有药物的羧酸，并加速支持药物开发的早期基于碳的 ADME 研究。
Zotero 插件