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Stereoselective Synthesis of Selected Potent ROMK Inhibitors (1)

有机合成与工艺文献分享 2025-06-06 07:38
文章摘要
本文主要探讨了针对ROMK抑制剂的立体选择性合成方法。研究背景涉及原有药物化学路线需要9步合成，过程复杂。研究目的是通过优化合成路线，提高效率和产量。研究过程中发现三氟甲磺酸衍生物15可大量商业获取，并尝试了多种反应条件，最终采用恶唑硼烷化学和钯介导的羰基化反应成功制备关键中间体16。由于游离碱8a的还原胺化反应效果不佳，研究转向SN2反应路径。结论表明通过路线优化可以更高效地合成目标ROMK抑制剂。
Stereoselective Synthesis of Selected Potent ROMK Inhibitors (1)
查看文献： Development of a Scalable Stereoselective Synthesis of Selected Potent ROMK Inhibitors
查看期刊： Organic Process Research & Development
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