Efficient, Scalable Synthesis of Functionalized Pyrrolo[2,1-f][1,2,4]triazines,Organic Process Research & Development

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Efficient, Scalable Synthesis of Functionalized Pyrrolo[2,1-f][1,2,4]triazines
Organic Process Research & Development ( IF 3.1 ) Pub Date : 2024-05-07 , DOI: 10.1021/acs.oprd.4c00116
Shawn K. Pack ₁ , Lei Feng ₂ , Ce Chen ₂ , Zhongzhen Li ₂

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An efficient, scalable synthesis of functionalized 5-fluoropyrrolo[2,1-f][1,2,4]triazines was developed from readily available starting materials. The synthesis is highlighted by a safe, Cu mediated difluoroacetate addition to vinyl TMS, selective formylation of a 3-fluoropyrrole, and sequential imine formation followed by cyclization to the triazine core. Addition of other electrophiles to 3-fluoropyrrole was also shown to be equally selective.

中文翻译：

高效、可规模化合成功能化吡咯并[2,1-f][1,2,4]三嗪

利用现成的起始材料开发了一种高效、可规模化的官能化 5-氟吡咯并[2,1-f][1,2,4]三嗪合成方法。该合成的特点是安全、铜介导的二氟乙酸加成到乙烯基 TMS、3-氟吡咯的选择性甲酰化以及顺序亚胺形成，然后环化为三嗪核心。向 3-氟吡咯添加其他亲电子试剂也显示出同样的选择性。

更新日期：2024-05-07

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