A modular, two-pot assembly of 7-arylpyrazolo[1,5-a]pyrimidones from aryl/heteroaryl halides and aminopyrazoles in library format was developed. Sonogashira coupling of aryl bromides with triethyl orthopropiolate, followed by in situ orthoester hydrolysis, provides access to β-aryl ynoates, which undergo regioselective cyclocondensation with aminopyrazoles. The ability to vary the C7 vector of 7-arylpyrazolo[1,5-a]pyrimidones in two steps using readily available (hetero)aryl halides significantly enhances synthetic access to this challenging vector.

中文翻译：

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7-（杂）芳基吡唑并[1,5 - a ]嘧啶-5-酮的并行方法

开发了以库形式从芳基/杂芳基卤化物和氨基吡唑类化合物合成的，由两锅组成的7-芳基吡唑并[1,5- a ]嘧啶酮的模块式两锅组件。芳基溴化物与原丙酸三乙酯的Sonogashira偶联，然后原位原酸酯水解，可提供β-芳基酸酯，后者与氨基吡唑进行区域选择性环缩合。使用易于获得的（杂）芳基卤化物分两步改变7-芳基吡唑并[1,5- a ]嘧啶的C7载体的能力显着增强了该挑战性载体的合成途径。