State Key Laboratory of Applied Organic Chemistry, College of Chemistry and Chemical Engineering, Lanzhou University , 222 Tianshui Nanlu, Lanzhou 730000, China.
College of Chemistry and Chemical Engineering, Liaocheng University , Liaocheng 252059, China.
Org Lett. 2017 Jun 2;19(11):2965-2968. doi: 10.1021/acs.orglett.7b01202. Epub 2017 May 17.
A novel Au-catalyzed [2 + 3] annulation reaction of enamides with propargyl esters has been developed, providing a new method for expeditious assembly of synthetically useful functionalized 1-azaspiro[4.4]nonane building blocks. Based on this key annulation, strategic installation of the pivotal azaspirocyclic core, followed by constructing the benzazepine unit via Witkop cyclization, led to the divergent total syntheses of cephalotaxine and cephalezomine H.
一种新型的 Au 催化的烯酰胺与丙炔酸酯的[2 + 3]环加成反应已经被开发出来，为快速构建合成有用的功能化 1-氮杂螺[4.4]壬烷砌块提供了一种新方法。基于这个关键的环加成反应，通过战略安装关键的氮杂螺环核心，然后通过 Witkop 环化构建苯并氮杂卓单元，实现了 Cephalotaxine 和 Cephalezomine H 的发散性全合成。
