通用一锅两步法获得具有高度骨架多样性的一系列新型多环杂环化合物。
General one-pot, two-step protocol accessing a range of novel polycyclic heterocycles with high skeletal diversity.
机构信息
College of Pharmacy, The University of Arizona, Oro Valley, 85737, United States.
出版信息
ACS Comb Sci. 2012 Aug 13;14(8):460-4. doi: 10.1021/co300046r. Epub 2012 Jul 12.
Abstract
An Ugi one-pot three-component four-center reaction was coupled with a subsequent acid mediated cyclodehydration step to furnish a multitude of unique scaffolds having in common an embedded or attached benzimidazole and often a ring system formed through lactamization. Using combinations of tethered Ugi inputs typically via tethered acid-ketone inputs and supporting reagents containing masked internal nucleophiles, such scaffolds were produced in good to excellent yields in an operationally friendly manner.
摘要
一种 Ugi 一锅三组分四中心反应与随后的酸介导的环脱水步骤相结合，提供了许多具有共同特点的独特支架，这些支架通常具有嵌入式或附着的苯并咪唑，并且经常通过内酰胺化形成环系统。通过通常使用连接的酸酮输入的组合以及含有掩蔽内部亲核试剂的支持试剂，以操作友好的方式以良好至优异的产率生产了这些支架。
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