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Development of a Manufacturing Process for S-892216 (2)

有机合成与工艺文献分享 2025-09-09 07:17
文章摘要
本文背景为药物S-892216的制造工艺开发，涉及多步有机合成反应优化。研究目的旨在通过筛选溶剂体系、添加剂和氯化试剂，建立高效稳定的生产工艺。关键发现包括：磺酸烷作为理想溶剂可同时溶解中间体；水/HCl添加剂与POCl3协同作用可生成更高活性的(HO)POCl2；采用(PhO)POCl2允许更高反应温度；溴乙腈被确定为最佳氰甲基化试剂。最终成功开发出六步合成工艺，总收率达41.3%，实现了从易得原料高效生产高质量目标产物。
Development of a Manufacturing Process for S-892216 (2)
查看文献： Development of a Manufacturing Process for S-892216 Part I: A Novel Method for Constructing a Multi-Substituted Barbiturate Skeleton for Scalable Synthesis
查看期刊：Organic Process Research & Development
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