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Rh(I)-Catalyzed C–H Functionalization Sequence

有机合成与工艺文献分享 2025-03-24 08:52

文章摘要

本文报道了Rh催化的C-H官能化反应，用于大规模合成取代四氢吡啶。研究首先在α,β-不饱和亚胺5上进行C-H活化，随后加入炔烃6形成氮杂三烯7，经过电环化反应生成8，最后通过氢化物供体和乙酸还原得到四氢吡啶9。经过优化，研究开发了两组反应条件：一组需要在手套箱中进行，使用对水分敏感的催化剂[RhCl(coe)2]2；另一组则使用空气稳定的催化剂[RhCl(cod)]2，可在实验室台面上进行。研究还展示了这两种反应条件在四个例子中的适用性，并在1克和20克规模上进行了反应，均获得了较高的产率。最终，研究证明了这种方法的效率和成本效益。

Rh(I)-Catalyzed C–H Functionalization Sequence

查看文献： Preparative Synthesis of Highly Substituted Tetrahydropyridines via a Rh(I)-Catalyzed C–H Functionalization Sequence
查看期刊：Organic Process Research & Development

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