Institut des sciences et ingénierie chimiques Ecole Polytechnique Fédérale de Lausanne (EPFL), CH-1015 Lausanne (Switzerland).
Angew Chem Int Ed Engl. 2014 Nov 17;53(47):12876-9. doi: 10.1002/anie.201407689. Epub 2014 Sep 26.
N-methylation of amines is an important step in the synthesis of many pharmaceuticals and has been widely applied in the preparation of other key intermediates and chemicals. Therefore, the development of efficient methylation methods has attracted considerable attention. In this respect, carbon dioxide is an attractive C1 building block because it is an abundant, renewable, and nontoxic carbon source. Consequently, we developed a highly chemoselective, metal-free catalytic system that operates under ambient conditions for the N-methylation of amines.
胺的 N-甲基化是许多药物合成中的重要步骤,并且已广泛应用于其他关键中间体和化学品的制备中。因此,开发高效的甲基化方法引起了相当大的关注。在这方面,二氧化碳是一种有吸引力的 C1 构建块,因为它是一种丰富、可再生且无毒的碳源。因此,我们开发了一种在环境条件下高化学选择性、无金属催化体系,用于胺的 N-甲基化。