A facile pseudo three component reaction for the synthesis of benzo [4,5]imidazo[1,2-a]pyridine derivatives

Gnanasamb, Amirthalingam Vasuki, N. Nithya
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Abstract

The benzimidazole moiety is amongst the diversely active scaffolds as antifungal, antibacterial, antiviral, anticancer and antimalarial agents.1‒4 Therefore, developing new approaches towards the synthesis of benzimdazole fused heterocycles have always been on need.5 Also, indeno and isoquinolino fused heterocycles have gained greater attention because of their medicinal and synthetic importance over years and the broad range of biological activity.6‒8 Therefore, benzimidazole fused indene, pyridine or isoquinoline are of great interest in general and many synthetic procedures are available till date.1 Moved by these results we desired to achieve a facile general synthetic protocol to obtain these diverse molecules. Multicomponent reaction has always proved to be a versatile tool towards the synthesis of structurally diverse and complex heterocycles in simple one pot manner.9 Our research group is actively engaged in developing multi-component reaction protocols for the synthesis of skeletally diverse, functionalized and biologically relevant small heterocyclic hybrids.10‒12 We report a simple and rapid procedure for the preparation of benzo[4,5]imidazo[1,2a]pyridines (Figure 2) with 2-(1H-benzo[d]imidazol-2-yl)acetonitrile.
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合成苯并[4,5]咪唑[1,2- A]吡啶衍生物的简易伪三组分反应
苯并咪唑部分是作为抗真菌、抗菌、抗病毒、抗癌和抗疟疾剂的多种活性支架之一。因此,开发苯并咪唑类杂环化合物的合成新方法一直是迫切需要的近年来,吲哚和异喹啉类杂环化合物因其广泛的生物活性以及在医学和合成方面的重要性而受到越来越多的关注。6-8因此,苯并咪唑融合茚、吡啶或异喹啉通常引起人们极大的兴趣,迄今已有许多合成方法受到这些结果的感动,我们希望实现一种简单的通用合成方案来获得这些不同的分子。多组分反应一直被证明是用简单的一锅法合成结构多样、复杂的杂环化合物的万能工具我们的研究小组积极致力于开发多组分反应方案,用于合成骨架多样化,功能化和生物相关的小杂环杂化物。我们报道了一种用2-(1h -苯并[d]咪唑-2-基)乙腈制备苯并[4,5]咪唑[1,2a]吡啶(图2)的简单快速方法。
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