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A Mild and Efficient Process for Ir-Catalyzed N‑Alkylation

有机合成与工艺文献分享 2025-07-04 07:59
文章摘要
本文研究了Ir催化的N-烷基化反应，旨在高效合成药物中间体吡啶-2-胺的N-烷基化产物。研究团队最初尝试了酰胺脱氧还原法，但未能成功，转而采用过渡金属催化策略。通过系统优化反应条件，包括碱、温度和催化剂用量，成功抑制了杂质7的生成。研究发现，反应温度对反应速率有显著影响，并通过ReactIR研究证实了反应过程中醛中间体的形成。最终，研究团队开发了高效的后处理步骤，获得了高产率且低Ir残留的目标产物，适用于下游转化。
A Mild and Efficient Process for Ir-Catalyzed N‑Alkylation
查看文献： Development of a Mild and Efficient Process for Ir-Catalyzed N-Alkylation of 4-Bromopyridin-2-amine with a Primary Alcohol via Borrowing Hydrogen
查看期刊： Organic Process Research & Development
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