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Optimized Synthesis of an Abemaciclib Intermediate

有机合成与工艺文献分享 2025-03-04 14:28
文章摘要
本文报道了Abemaciclib中间体的优化合成方法。研究背景基于Miyaura硼酸化反应中存在的副产物问题，研究目的是通过优化反应条件减少副产物的生成并提高反应效率。通过筛选不同的碱和配体，研究发现改变碱的种类对反应速率的提升有显著影响。最终优化的反应条件不仅大幅减少了芳基重排副反应，还提高了反应速率和产率。结论表明，优化后的条件使得Abemaciclib中间体的合成产率提高了6%，反应时间减少了14小时，钯催化剂用量减少了50%。
Optimized Synthesis of an Abemaciclib Intermediate
查看文献： Optimized Synthesis of an Abemaciclib Intermediate: Improved Conditions for a Miyaura Borylation/Suzuki Coupling Process
查看期刊： Organic Process Research & Development
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