Graduate School of Pharmaceutical Sciences, The University of Tokushima, 1-78-1 Sho-machi, Tokushima 770-8505 (Japan).
Angew Chem Int Ed Engl. 2014 Dec 22;53(52):14550-4. doi: 10.1002/anie.201409015. Epub 2014 Oct 29.
A novel strategy for the one-pot synthesis of substituted pyridines from N-arylmethyl 3-aziridinylpropiolate esters is described. The method employs a three-step procedure including the formation of allenyl imines, phosphine-catalyzed cyclization, and subsequent oxidation of the dihydropyridines. Depending on the reaction conditions of the final oxidation step, tri- and tetrasubstituted pyridines can be selectively produced.
描述了一种从 N-芳基甲基 3-氮丙啶基丙炔酸酯一锅法合成取代吡啶的新策略。该方法采用三步法，包括烯基亚胺的形成、膦催化环化和随后的二氢吡啶氧化。根据最终氧化步骤的反应条件，可以选择性地生成三取代和四取代吡啶。
