A sustainable and chemoselective continuous flow hydrogenation of functionalized 2-azetines to azetidines

Elena Graziano , Debora Cannillo , Mauro Spennacchio , Pantaleo Musci , Luisa Pisano , Michael Andresini , Marco Colella
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引用次数: 3

Abstract

The synthesis of functionalized azetidines from azetines is poorly explored. Here, we report the safe and sustainable continuous flow hydrogenation of 2-azetines using ethyl acetate and CPME as environmentally responsible solvents. The chemoselective saturation of the endocyclic double bond of 2-azetines bearing additional functional groups sensitive to hydrogenation has been additionally disclosed. Moreover, the protocol has been successfully combined with the continuous flow preparation of the substrates, accessing to a bio-relevant azetidine through a telescoped multistep approach.

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一种可持续的化学选择性连续流加氢制备氮杂环丁烷
由氮杂环丁烷合成功能化氮杂环丁烷的研究进展缓慢。在这里,我们报道了使用乙酸乙酯和CPME作为对环境负责的溶剂安全和可持续地连续流动氢化2-ζ。另外还公开了具有对氢化敏感的附加官能团的2-ζ的内环双键的化学选择性饱和。此外,该方案已成功地与底物的连续流动制备相结合,通过伸缩式多步骤方法获得生物相关的氮杂环丁烷。
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