一种通过 2-乙炔苯胺、磺酰基叠氮化物和硝基烯烃的三组分反应制备多取代吲哚的简便方法。
A facile route to polysubstituted indoles via three-component reaction of 2-ethynylaniline, sulfonyl azide, and nitroolefin.
机构信息
Department of Chemistry, Fudan University, Shanghai, China.
出版信息
Org Lett. 2011 Mar 4;13(5):848-51. doi: 10.1021/ol102775s. Epub 2011 Feb 7.
PMID:21299243
Abstract
A copper-catalyzed three-component reaction of 2-ethynylaniline, sulfonyl azide, and nitroolefin is reported. This reaction generates functionalized indoles in good yields and proceeds smoothly under mild conditions. Some hits as an HCT-116 inhibitor are found from the preliminary biological screening.
摘要
本文报道了一种铜催化的 2-乙炔基苯胺、磺酰基叠氮化物和硝基烯烃的三组分反应。该反应在温和条件下以良好的收率生成功能化吲哚，且反应过程平稳。初步的生物筛选发现一些化合物具有 HCT-116 抑制剂的活性。
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