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Evolution of the Synthesis Route for CC-99677 (2)

有机合成与工艺文献分享 2025-12-26 08:16
文章摘要
本文背景涉及药物中间体CC-99677的合成路线优化。研究目的是开发一条更简洁、高效的合成路径，以替代原有存在问题的化学步骤，并探索关键反应步骤（如Heck/环化、区域选择性O-烷基化）的改进条件。结论表明，通过降低钯催化剂负载至0.5-1.0 mol%可完成Heck偶联，但完全转化需要1-3 mol%催化剂或引入酸催化剂促进异构化；同时，研究发现t-BuOLi/DMPU条件适用于商业工艺的第一步，而区域选择性O-苯甲基化可通过钯催化实现，为合成提供了更优方案。
Evolution of the Synthesis Route for CC-99677 (2)
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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