Song J J, Yee N K
Department of Chemical Development, Boehringer Ingelheim Pharmaceuticals, Inc., Ridgefield, Connecticut 06877-0368, USA.
Org Lett. 2000 Feb 24;2(4):519-21. doi: 10.1021/ol990409x.
[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.
[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。