School of Pharmaceutical Sciences, South-Central University for Nationalities, Wuhan 430074, China.
J Org Chem. 2021 Jan 1;86(1):559-573. doi: 10.1021/acs.joc.0c02244. Epub 2020 Dec 10.
An efficient [3 + 2] cycloaddition of in situ generated nitrile imines with enamides has been established. A wide range of functionalized pyrazoline derivatives (53 examples) were obtained in moderate to good yields (up to 96%) under very mild conditions. This protocol features broad substrate scope, good functional group tolerance, and operational simplicity. Practical transformation of the products into useful pyrazoles via a one-pot process and the scalability of this protocol highlight the utility of this synthetic methodology.
一种高效的原位生成的腈亚胺与烯酰胺的[3+2]环加成反应已经建立。在非常温和的条件下，该反应以中等至良好的收率（高达 96%）得到了广泛的功能化吡唑啉衍生物（53 个实例）。该方案具有广泛的底物范围、良好的官能团耐受性和操作简单性。通过一锅法将产物转化为有用的吡唑，并对该方案进行了扩大规模，突出了这种合成方法的实用性。
