英语翻译Inexpensive copper catalysts allow for efficient syntheses of N-aryl-,N-acyl-,or N-H-(aza)indoles starting from ortho-alkynylbromoarenes.The broad scope of this domino N-arylation/hydro-ACHTUNGTRENUNGamin(d)ation process is highlighted by

英语翻译Inexpensive copper catalysts allow for efficient syntheses of N-aryl-,N-acyl-,or N-H-(aza)indoles starting from ortho-alkynylbromoarenes.The broad scope of this domino N-arylation/hydro-ACHTUNGTRENUNGamin(d)ation process is highlighted by
英语翻译
Inexpensive copper catalysts allow for efficient syntheses of N-aryl-,N-acyl-,or N-H-(aza)indoles starting from ortho-alkynylbromoarenes.The broad scope of this domino N-arylation/hydro-ACHTUNGTRENUNGamin(d)ation process is highlighted by the synthesis of highly functionalized indoles,as well as of a Chek1/KDR inhibitor pharmacophore
Notably,ortho-substituents on more sterically hindered aniline derivatives
were well tolerated (entries 7,and 8),as were chlorides as functionalities,which resulted in the chemoselective preparation of substituted indoles 3i–3k (entries
9–11).As to the mechanism of this “nitrogen ligand-free” copper-catalyzed transformation,experiments with a secondary amine suggest a reaction sequence
consisting of intermolecular hydroamination,followed by intramolecular N-arylation.
Support by the DFG,the DAAD (fellowship to HKP),the GIF,and Sanofi-Aventis is gratefully acknowledged.

英语翻译Inexpensive copper catalysts allow for efficient syntheses of N-aryl-,N-acyl-,or N-H-(aza)indoles starting from ortho-alkynylbromoarenes.The broad scope of this domino N-arylation/hydro-ACHTUNGTRENUNGamin(d)ation process is highlighted by
廉价的铜催化剂可高效合成N -芳基,N -酰基,或NH - （AZA ）吲哚alkynylbromoarenes邻开始.这个多米诺骨牌N-arylation/hydro-ACHTUNGTRENUNGamin （D） ATION过程的范围广泛,是突出的高功能化吲哚的合成,以及作为一个Chek1/KDR抑制剂药效
值得注意的是,邻位取代基的空间位阻的苯胺衍生物
良好的耐受性（条目7和8） ,以及作为功能的氯化物,这导致在化学选择性制备取代吲哚3I - 3K （条目
9-11） .这一机制的“氮配体自由”铜催化转化,与二级胺的实验表明反应序列
由分子hydroamination组成,其次是分子内的N -芳基化.
东风集团的支持, （ DAAD的奖学金,以香港邮政） , GIF ,赛诺菲 - 安万特公司表示感谢.