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Process Intensive Synthesis of Propofol Enabled by Continuous Flow Chemistry
Organic Process Research & Development ( IF 3.4 ) Pub Date : 2022-06-23 , DOI: 10.1021/acs.oprd.1c00416
Laurent Vinet 1 , Lorenzo Di Marco 1 , Vanessa Kairouz 1 , André B. Charette 1
Affiliation  

A multi-step process using continuous flow chemistry to produce propofol is described. A scale-up of a 5-stage process (two continuous flow chemical steps, two extractions using a semi-batch approach, and one purification) provided propofol in high purity. This process minimizes the number of impurities formed during the double Friedel–Crafts reaction allowing to run two continuous flow chemical steps sequentially. The use of simple, inexpensive, and readily available reagents affords a viable process for this widely employed active pharmaceutical ingredient.

中文翻译:

通过连续流动化学实现丙泊酚的工艺密集合成

描述了使用连续流动化学生产丙泊酚的多步骤工艺。一个 5 阶段工艺(两个连续流动化学步骤、两个使用半间歇方法的萃取和一个纯化)的放大提供了高纯度的丙泊酚。该过程最大限度地减少了双傅克反应过程中形成的杂质数量,从而允许依次运行两个连续流动的化学步骤。使用简单、廉价和容易获得的试剂为这种广泛使用的活性药物成分提供了可行的方法。
更新日期:2022-06-23
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