Convenient Continuous Flow Synthesis of N-Methyl Secondary Amines from Alkyl Mesylates and Epoxides,Organic Process Research & Development

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Convenient Continuous Flow Synthesis of N-Methyl Secondary Amines from Alkyl Mesylates and Epoxides
Organic Process Research & Development ( IF 3.1 ) Pub Date : 2020-08-25 , DOI: 10.1021/acs.oprd.0c00193
Gary Mathieu ₁ , Heena Patel ₁ , Hélène Lebel ₁

Affiliation

The first continuous flow process was developed to synthesize N-methyl secondary amines from alkyl mesylates and epoxides via a nucleophilic substitution using aqueous methylamine. A variety of N-methyl secondary amines were produced in good to excellent yields, including a number of bioactive compounds or their precursors. Up to 10.6 g (88% yield) of an N-methyl secondary amine was produced in 140 min process time. The amination procedure included an in-line workup, and the starting mesylate material was also produced in continuous flow from the corresponding alcohol. Finally, an in-line process combining the mesylate synthesis and nucleophilic substitution was developed.

中文翻译：

从烷基甲磺酸酯和环氧化物方便连续连续合成N-甲基仲胺

开发了第一连续流方法，以使用甲胺水溶液经由亲核取代从烷基甲磺酸酯和环氧化物合成N-甲基仲胺。以良好至优异的产率生产了多种N-甲基仲胺，包括许多生物活性化合物或其前体。在140分钟的处理时间内产生了多达10.6 g（88％的产率）的N-甲基仲胺。胺化过程包括在线后处理，并且甲磺酸酯原料也由相应的醇连续流产生。最后，开发了一种结合甲磺酸酯合成和亲核取代的在线工艺。

更新日期：2020-10-17

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