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Evolution of the Synthesis Route for CC-99677 (1)

有机合成与工艺文献分享 2025-12-25 07:26
文章摘要
本文背景为CC-99677作为一种不可逆的丝裂原活化蛋白激酶激活蛋白激酶2抑制剂，在体外可持续减少促炎细胞因子的产生。研究目的是改进其合成路线，以提高产率、减少步骤并解决中间体稳定性问题。具体改进包括避免一次桑德迈尔反应，通过磺酰胺酯18引入手性氨基丙基侧链，并将喹啉氧化/重排序列提前以消除氧化前的Boc保护需求。结论表明，在NMP中使用叔丁醇锂效果最佳，转化率约90%；同时发现磺酰胺酯18在极性溶剂中稳定性有限，在非极性溶剂如MeTHF中稳定性更好。最终工艺通过将18溶于MeTHF并低温下加入21的NMP溶液，再缓慢加入LiOt-Bu的THF溶液，实现了≥95%的溶液产率。
Evolution of the Synthesis Route for CC-99677 (1)
查看文献： Evolution of the Synthesis Route for CC-99677: From Discovery toward Commercialization
查看期刊：Organic Process Research & Development
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