法国巴黎萨克雷大学Davide Audisio团队报道了药物可逆脱氰直接碳同位素交换的方法。 相关研究成果于2021年4月7日发表在国际知名学术期刊《美国化学会杂志》。

碳-14的加入可以追踪有机分子，并提供有关其命运的重要知识。这些信息在药物开发、作物科学和人类食品安全评估中至关重要。

该文描述了一种过渡金属催化的在芳香腈上实现碳同位素交换的方法。通过利用放射性标记的前体Zn（[14C]CN）2，该方案允许在单个步骤中插入所需的碳标记而无需结构修饰。通过降低合成成本和限制放射性废物的产生，这一程序将有助于含腈药物的标记，并加速基于14C的支持药物开发的ADME研究。

附：英文原文

Title: Direct Carbon Isotope Exchange of Pharmaceuticals via Reversible Decyanation

Author: Minghao Feng, Joao De Oliveira, Antoine Sallustrau, Gianluca Destro, Pierre Thuéry, Sebastien Roy, Thibault Cantat, Charles S. Elmore, Jorg Blankenstein, Frédéric Taran, Davide Audisio

Issue&Volume: April 7, 2021

Abstract: The incorporation of carbon-14 allows tracking of organic molecules and provides vital knowledge on their fate. This information is critical in pharmaceutical development, crop science, and human food safety evaluation. Herein, a transition-metal-catalyzed procedure enabling carbon isotope exchange on aromatic nitriles is described. By utilizing the radiolabeled precursor Zn([14C]CN)2, this protocol allows the insertion of the desired carbon tag without the need for structural modifications, in a single step. By reducing synthetic costs and limiting the generation of radioactive waste, this procedure will facilitate the labeling of nitrile containing drugs and accelerate 14C-based ADME studies supporting drug development.

DOI: 10.1021/jacs.1c01923

Source: https://pubs.acs.org/doi/10.1021/jacs.1c01923