To study the antikinetoplastid structure–activity relationships in a 3-nitroimidazo[1,2-a]pyridine series, we explored the substitution of positions 5 and 7 of the scaffold, developing nucleophilic aromatic substitution reactions and palladium-catalyzed Suzuki–Miyaura, Sonogashira, and Buchwald–Hartwig cross-coupling reactions that had never been reported at these positions in this series. In four steps from 2-amino(bromo)pyridines, 33 original compounds were obtained, allowing a better definition of the antiparasitic pharmacophore.

中文翻译：

---

使用 SNAr 和钯催化反应合成新的 5-或 7-取代 3-硝基咪唑并[1,2-a]吡啶衍生物以探索抗寄生虫结构-活性关系

为了研究 3-硝基咪唑并[1,2- a ]吡啶系列中的抗动质体结构-活性关系，我们探索了支架 5 和 7 位的取代，开发了亲核芳香取代反应和钯催化的 Suzuki-Miyaura, Sonogashira ，以及本系列中这些位置从未报道过的 Buchwald-Hartwig 交叉偶联反应。通过 2-氨基（溴）吡啶的四个步骤，获得了 33 种原始化合物，从而可以更好地定义抗寄生虫药效团。