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C−H Arylation in the Formation of BMS-911543

有机合成与工艺文献分享 2025-04-06 06:04
文章摘要
本文讨论了BMS-911543的合成路线改进。原路线存在中间体不稳定、反应条件苛刻以及铜残留问题。通过改进逆合成分析，研究者发明了一种钯催化的C−H官能化反应，实现了关键吡咯和咪唑片段的快速连接。pKa计算显示，仅需催化量的碱即可完成环化反应。实验发现NaOEt是最佳碱，室温下1小时内即可完成反应。进一步研究发现，使用NaOH作为碱可得到羧酸盐21作为唯一产物。使用Bu4NOH或Et4NOH可加快反应速率，并证实反应通过酯水解生成22，随后偶联得到羧酸盐21。
C−H Arylation in the Formation of BMS-911543
查看文献： C–H Arylation in the Formation of a Complex Pyrrolopyridine, the Commercial Synthesis of the Potent JAK2 Inhibitor, BMS-911543
查看期刊：Journal of Organic Chemistry
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