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Development of a Manufacturing Process for S-892216 (1)

有机合成与工艺文献分享 2025-09-08 07:36
文章摘要
本文背景为开发第二代3CL蛋白酶抑制剂S-892216的合成工艺，该药物是治疗SARS-CoV-2感染的临床候选药物。研究目的旨在解决传统巴比妥酸盐合成方法产率低的问题，通过探索新型合成路线和反应条件优化工艺。结论表明采用含2,4,6-三氯苯氧基的丙二酸衍生物与尿素反应，配合T3P活化剂和DBU催化剂，成功将关键中间体11的产率提升至67%，并解决了规模化生产中的操作难题，为药物工业化生产提供了可行方案。
Development of a Manufacturing Process for S-892216 (1)
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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