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Safe and Efficient Phosgenation Reactions in a Continuous Flow Reactor
Organic Process Research & Development ( IF 3.4 ) Pub Date : 2018-01-26 00:00:00 , DOI: 10.1021/acs.oprd.7b00353
Hiroaki Yasukouchi 1 , Akira Nishiyama 1 , Masaru Mitsuda 1
Affiliation  

Phosgene is widely used in organic synthesis owing to its high reactivity, utility, and cost efficiency. However, the use of phosgene in batch processes on the industrial scale is challenging owing to its toxicity. An effective method to minimize reaction volumes and mitigate the safety risks associated with hazardous chemicals is the use of flow reactors. Consequently, we have established a flow reaction system using triphosgene and tributylamine, which affords a homogeneous reaction that avoids clogging issues. In addition, we have demonstrated that this methodology can be applied to a wide variety of phosgene reactions, including the preparation of pharmaceutical intermediates, in good to excellent yields.

中文翻译:

连续流反应器中的安全高效的光气化反应

光气因其高反应性,实用性和成本效益而被广泛用于有机合成中。然而,由于光气的毒性,在工业规模的批量生产中使用光气具有挑战性。最小化反应体积并减轻与危险化学品有关的安全风险的有效方法是使用流动反应器。因此,我们建立了使用三光气和三丁胺的流动反应系统,该系统可提供均相反应,避免发生堵塞问题。另外,我们已经证明,该方法可以良好的收率应用到各种各样的光气反应中,包括制备药物中间体。
更新日期:2018-01-26
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