通过α,β-不饱和酮与 2-硝基苯乙腈一锅串联反应快速获得α-咔啉类化合物及其产物的抗增殖活性。
Rapid access to α-carbolines via a one-pot tandem reaction of α,β-unsaturated ketones with 2-nitrophenylacetonitrile and the anti-proliferative activities of the products.
机构信息
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.
出版信息
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。
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