The first example of a sequential heterocycle formation/multicomponent reaction using an automated continuous flow microreactor assembly is reported. Consecutive Hantzsch thiazole synthesis, deketalization, and Biginelli multicomponent reaction provides rapid and efficient access to highly functionalized, pharmacologically significant 5-(thiazol-2-yl)-3,4-dihydropyrimidin-2(1H)-ones without isolation of intermediates. These complex small molecules are generated in reaction times less than 15 min and in high yields (39-46%) over three continuous chemical steps.

中文翻译：

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连续杂环/多组分反应的自动化过程：5-(噻唑-2-基)-3,4-二氢嘧啶-2(1H)-酮的多步连续流动合成。

报告了使用自动连续流动微反应器组件的顺序杂环形成/多组分反应的第一个例子。连续的 Hantzsch 噻唑合成、去缩酮化和 Biginelli 多组分反应可快速有效地获得高度功能化、具有药理学意义的 5-(thiazol-2-yl)-3,4-dihydropyrimidin-2(1H)-ones，无需分离中间体。这些复杂的小分子是在不到 15 分钟的反应时间内生成的，并且通过三个连续的化学步骤以高产率 (39-46%) 生成。