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Nitrileimines as an alternative to azides in base-mediated click [3 + 2] cycloaddition with methylene active nitriles
RSC Advances ( IF 3.9 ) Pub Date : 2020-4-3 , DOI: 10.1039/d0ra01417f
Mykola A Tupychak 1 , Olga Ya Shyyka 1 , Nazariy T Pokhodylo 1 , Mykola D Obushak 1
Affiliation  

Nitrileimines were implemented in practical click protocols with oxopropanenitriles for the straightforward 5-amino-1H-pyrazole synthesis via 1,3-dipolar cycloaddition. The reaction proceeds at room temperature in a short time with base catalysis and no chromatographic purification. High purity products were isolated by simple filtration. The selectivity of the reaction was observed.

中文翻译:


腈亚胺作为叠氮化物的替代物,用于与亚甲基活性腈进行碱介导的点击 [3 + 2] 环加成反应



腈亚胺在实际点击方案中与氧代丙腈一起实现,通过1,3-偶极环加成直接合成 5-氨基-1H-吡唑。该反应在室温下在碱催化下在短时间内进行,无需色谱纯化。通过简单过滤分离出高纯度产物。观察反应的选择性。
更新日期:2020-04-03
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