开发一个大规模的化工艺使用连续流化学路径,以合成的remdesivir
Tiago Vieira1, Andrew C Stevens1, Andrei Chtchemelinine2
1Gilead Alberta ULC, 1021 Hayter Road, Edmonton, Alberta T6S 1A1, Canada.
概括
连续流化学提高了危险的化反应的安全性和控制. 这种方法成功地用于合成候选药物remdesivir,克服了传统批处理的挑战.
科学领域:
- 有机化学 有机化学
- 过程化学 过程化学
- 药用化学 医学化学
背景情况:
- 由于危险的试剂和严格的参数要求 (例如冷温度),制造规模的化反应带来了重大安全和控制挑战.
- 传统的批量加工设备难以管理高效和选择性化所需的风险和精确条件.
- 连续流化学为处理危险反应和改善工艺控制提供了一个有希望的替代方案.
研究的目的:
- 为了证明连续流化学对于大规模的化反应的应用.
- 介绍一个用流化合成候选药物雷梅西维尔的案例研究.
- 突出流化学在减轻风险和加强对危险反应的控制方面的优势.
主要方法:
- 使用连续流反应堆系统实现化化学.
- 在流量设置中对选择性和转换反应参数的优化.
- 案例研究涉及化一种糖化物中间体用于雷梅西维尔合成.
主要成果:
- 连续流处理成功地减轻了与处理危险的化试剂相关的风险.
- 在流量系统中实现了对反应参数 (包括温度) 的增强控制.
- 糖化物中间体的化过程以可接受的选择性和转化进行,使得remdesivir合成成为可能.
结论:
- 连续流化学为工业规模的化提供了比批处理更安全,更可控的替代方案.
- 雷德西维尔中间体的成功合成展示了流化的实际实用性.
- 这种方法提高了制药生产过程的安全性和效率.
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