Abstract

A highly efficient PASE approach to a new class of polycyclic purine derivatives has been proposed. The strategy includes a consecutive reduction, auto-aromatization, and heterocyclization of the initial nitrobenzimidazopyrimidines obtained by a three-component condensation. It was shown that reduction of nitrobenzimidazopyrimidines by metals in acidic media was more efficient than heterogeneous hydro­genation. Novel derivatives of benz[4,5]imidazo[1,2-a]purines were obtained­ in good yields and the proposed structure was confirmed by X-ray crystal structure analysis. The obtained convergent benzimidazopurines combine two relevant medicinal chemistry scaffolds – benz­imidazole and purine.

中文翻译：

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用PASE方法合成苯并咪唑嘌呤类缩聚嘌呤衍生物

摘要

已经提出了一种用于新型多环嘌呤衍生物的高效PASE方法。该策略包括通过三组分缩合获得的初始硝基苯并咪唑并嘧啶的连续还原，自动芳构化和杂环化。结果表明，金属在酸性介质中还原硝基苯并咪唑并嘧啶比异质氢化更有效。以高收率获得了苯并[4,5]咪唑并[1,2- a ]嘌呤的新型衍生物，并通过X射线晶体结构分析证实了所提出的结构。获得的会聚苯并咪唑嘌呤会结合两种相关的药物化学支架–苯并咪唑和嘌呤。