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Development of a continuous flow synthesis of propranolol: tackling a competitive side reaction
Journal of Flow Chemistry ( IF 2.7 ) Pub Date : 2019-08-14 , DOI: 10.1007/s41981-019-00047-8
Sonia De Angelis , Paolo Celestini , Rosa Purgatorio , Leonardo Degennaro , Gabriele Rebuzzini , Renzo Luisi , Claudia Carlucci

This work reports the preparation of propranolol according to a flow process. Propranolol has been prepared paying attention to tackle the formation of the by-product tertiary amine, resulting from an additional ring opening of the starting epoxide. Remarkably, the use of catalytic amount of water resulted beneficial for the yield and purity of the desired propranolol, and to substantially reducing the amount of tertiary amine byproduct. The high concentration of the solutions allowed for a productivity of several grams/h.



中文翻译:

普萘洛尔连续流动合成的开发:解决竞争性副反应

这项工作报告了根据流动过程普萘洛尔的制备。制备普萘洛尔时要特别注意处理由于起始环氧化物的额外开环而引起的副产物叔胺的形成。值得注意的是,使用催化量的水有利于所需普萘洛尔的收率和纯度,并大大减少了叔胺副产物的量。溶液的高浓度允许几克/小时的生产率。

更新日期:2019-08-14
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