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Metal-free one-pot synthesis of benzofurans with ynones and quinones through aza-Michael/Michael/annulation sequence
Tetrahedron ( IF 2.1 ) Pub Date : 2017-11-10 , DOI: 10.1016/j.tet.2017.11.014
Hai-Lei Cui , Hui-Qing Deng , Jin-Ju Lei

A convenient metal-free one-pot synthesis of benzofuran derivatives starting from simple ynones has been developed. Various functionalized benzofurans closely related to bioactive molecules can be obtained in moderate to good yields (up to 90%) through aza-Michael/Michael/annulation sequence. Preparative scale synthesis of benzofurans has also been successfully achieved. The application of the benzofuran products has been shown by easy transformations to highly functionalized molecules holding significant promise for medicinal chemistry and organic material chemistry.



中文翻译:

通过aza-Michael / Michael / annulation序列,无金属一锅法合成含苯并呋喃酮与醌和醌

已经开发了一种方便的无金属一锅合成苯并呋喃衍生物的方法,该方法可从简单的炔酮开始。可以通过aza-Michael / Michael / annulation序列以中等到良好的产率(高达90%)获得与生物活性分子密切相关的各种功能化的苯并呋喃。苯并呋喃的制备规模合成也已成功实现。苯并呋喃产品的应用已通过轻松转化为高度功能化的分子得到了展示,这对药物化学和有机材料化学具有重大的前景。

更新日期:2017-11-10
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