二乙基锌催化的炔基磺酰胺分子内氢胺化反应及相关串联环化/加成反应。
Et2Zn-catalyzed intramolecular hydroamination of alkynyl sulfonamides and the related tandem cyclization/addition reaction.
作者信息
Yin Yan, Ma Wenying, Chai Zhuo, Zhao Gang
机构信息
Laboratory of Modern Synthetic Organic Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, 354 Fenglin Lu, Shanghai 200032, China.
出版信息
J Org Chem. 2007 Jul 20;72(15):5731-6. doi: 10.1021/jo070681h. Epub 2007 Jun 20.
Intramolecular hydroamination of alkynyl amides was effected by a catalytic amount of Et2Zn (20 mol %) to form indole derivatives, and a tandem cyclization/nucleophilic addition procedure involving reaction of the indole zinc salt intermediate with acid chlorides or halides was developed to provide an efficient approach to C3-substituted indole derivatives when an excess of Et2Zn (120 mol %) was used.
在催化量的二乙基锌（20摩尔%）作用下，炔基酰胺发生分子内氢胺化反应生成吲哚衍生物；当使用过量的二乙基锌（120摩尔%）时，开发了一种串联环化/亲核加成方法，该方法涉及吲哚锌盐中间体与酰氯或卤化物的反应，为制备C3-取代的吲哚衍生物提供了一种有效途径。
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