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Synthesis of Dolutegravir Exploiting Continuous Flow Chemistry
The Journal of Organic Chemistry ( IF 3.6 ) Pub Date : 2023-08-08 , DOI: 10.1021/acs.joc.3c01365
Sinazo Nqeketo 1 , Paul Watts 1
Affiliation  

An efficient continuous flow process for the synthesis of dolutegravir, an active pharmaceutical ingredient (API) for HIV treatment, was investigated. The synthetic procedure starts from a readily available benzyl-protected pyran via six chemical transformations using continuous flow reactors. The significant advantage of this flow process includes the reduction of the overall reaction time from 34.5 h in batch to 14.5 min. The overall yield of each reaction step improved dramatically upon flow optimization. Another key feature of this synthesis is telescoping multiple steps.

中文翻译:

利用连续流化学合成多替拉韦

研究了一种用于合成多替拉韦(一种用于治疗 HIV 的活性药物成分 (API))的高效连续流程。合成过程从易于获得的苄基保护的吡喃开始,通过连续流动反应器进行六次化学转化。该流程的显着优势包括将总反应时间从批量的 34.5 小时减少到 14.5 分钟。通过流程优化,每个反应步骤的总产率显着提高。该合成的另一个关键特征是伸缩多个步骤。
更新日期:2023-08-10
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