The reactivity and synthesis of new analogues of pyrido[1,2-a]benzimidazoles have been explored. Twenty-three derivatives bearing phenoxy, thiophenoxy, aniline, and aryl groups at the 1-position were successfully synthesised in 25–91 % yield, via nucleophilic substitution, Buchwald–Hartwig amination, and Suzuki coupling type processes. Solvent free synthetic protocols were employed to achieve the nucleophilic substitution of anilines with electron donating groups or moderately electron withdrawing groups on a sterically demanding intermediate (7a). An unusual polycyclic heterocycle was identified as a side-product during this work: a dimeric bis(pyrido[1,2-a]benzimidazole).

已经研究了吡啶并[1,2- a ]苯并咪唑的新类似物的反应性和合成。通过亲核取代，Buchwald-Hartwig胺化和Suzuki偶联类型工艺，成功合成了1位上带有苯氧基，噻吩氧基，苯胺和芳基的23种衍生物，收率25-91％。采用无溶剂的合成方案，通过空间需求中间体（7a）上的供电子基团或适度吸电子基团实现苯胺的亲核取代。在这项工作期间，一个不寻常的多环杂环被鉴定为副产物：二聚双（吡啶并[1,2- a ]苯并咪唑）。