State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zu Chong Zhi Road, Shanghai, 201203, P.R. China.
Org Biomol Chem. 2014 Jan 14;12(2):355-61. doi: 10.1039/c3ob41921e.
An effective and convenient method has been developed for the preparation of 2 or 2,4-substituted α-carbolines via a one-pot tandem reaction of α,β-unsaturated ketones with 2-nitrophenylacetonitrile in the presence of zinc dust, acetic acid and triethylamine. This protocol presents a simple, rapid and pot/step economical strategy for preparing biologically interesting α-carbolines with moderate anti-tumor activities.
现已开发出一种有效且便捷的方法，通过在锌粉、乙酸和三乙胺存在下，使α,β-不饱和酮与 2-硝基苯乙腈一锅串联反应，可制备 2 位或 2,4-位取代的α-咔啉。该方案为具有中等抗肿瘤活性的生物相关α-咔啉提供了一种简单、快速和节省釜/步的策略。
