通过钯催化的分子内胺化反应合成2-芳基-2H-吲唑的新方法。
A novel synthesis of 2-aryl-2H-indazoles via a palladium-catalyzed intramolecular amination reaction.
作者信息
Song J J, Yee N K
机构信息
Department of Chemical Development, Boehringer Ingelheim Pharmaceuticals, Inc., Ridgefield, Connecticut 06877-0368, USA.
出版信息
Org Lett. 2000 Feb 24;2(4):519-21. doi: 10.1021/ol990409x.
PMID:10814366
Abstract
[reaction: see text] A variety of 2-aryl-2H-indazoles were synthesized by the palladium-catalyzed intramolecular amination of the corresponding N-aryl-N(o-bromobenzyl)hydrazines. Of several sets of reaction conditions surveyed, the combination of Pd(OAc)2/dppf/tBuONa gave the best results. This method applies to a wide scope of substrates containing electron-donating and electron-withdrawing substituents.
摘要
[反应：见正文] 通过钯催化相应的N-芳基-N（邻溴苄基）肼的分子内胺化反应合成了多种2-芳基-2H-吲唑。在所研究的几组反应条件中，Pd（OAc）2/dppf/tBuONa的组合效果最佳。该方法适用于含有供电子和吸电子取代基的广泛底物。
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