Zhu Lin, Xiong Yan, Li Chaozhong
†Department of Chemistry, University of Science and Technology of China, Hefei, Anhui 230026, P. R. China.
‡Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, 345 Lingling Road, Shanghai 200032, P. R. China.
J Org Chem. 2015 Jan 2;80(1):628-33. doi: 10.1021/jo502265a. Epub 2014 Nov 26.
We report herein a facile synthesis of α-methylene-β-lactams. Thus, under the catalysis of triphenylphosphine, a number of 2-propiolamidoacetates or α-propiolamido ketones in refluxing ethanol underwent umpolung cyclization to afford the corresponding 4-substituted 3-methyleneazetidin-2-ones in high yields.
我们在此报告一种简便合成α-亚甲基-β-内酰胺的方法。因此，在三苯基膦催化下，多种2-丙炔酰胺基乙酸酯或α-丙炔酰胺基酮在回流乙醇中进行极性翻转环化反应，以高产率得到相应的4-取代-3-亚甲基氮杂环丁烷-2-酮。
