A highly active catalyst for the reductive cyclization of ortho-nitrostyrenes under mild conditions
摘要:
A mild and efficient method for the palladium-Catalyzed reductive Cyclization of ortho-nitrostyrenes to afford indoles is reported. \Treatment of ortho-nitrostyrenes with 0.1 mol% palladium (II) trifluoracetate [Pd(TFA)(2)] and 0.7 mol% 3.4,7,8-tetramethyl-1,10-phenanthroline (tm-phen) in DMF at 15 psig CO and 80 degrees C afforded indoles in good to excellent yields. When the reaction was conducted in toluene. the corresponding N-hydroxyindole was isolated. A mechanism that accounts for the formation of N-hydroxyindole is proposed. (c) 2005 Elsevier Ltd. All rights reserved.
Rapid and Efficient Synthesis of 1H-Indol-2-yl-1H-quinolin-2-ones
摘要:
A concise and efficient synthesis of the novel indol-2-yl-1H-quinolin-2-one ring system found in the potent and selective KDR kinase inhibitors 1-3 is presented.
Substituted indoles and a process for preparing substituted indoles
申请人:Davies W Ian
公开号:US20070054921A1
公开(公告)日:2007-03-08
The instant invention is directed to novel compounds of Formulae (I) and (II), as wells a process for preparing compounds of Formula (II). The process comprises a palladium-catalyzed reductive cyclization of a compound of Formula (I) to produce a compound of Formula (II).
A highly active catalyst for the reductive cyclization of ortho-nitrostyrenes under mild conditions
作者:Ian W. Davies、Jacqueline H. Smitrovich、Rick Sidler、Chuanxing Qu、Venita Gresham、Charles Bazaral
DOI:10.1016/j.tet.2005.03.142
日期:2005.6
A mild and efficient method for the palladium-Catalyzed reductive Cyclization of ortho-nitrostyrenes to afford indoles is reported. \Treatment of ortho-nitrostyrenes with 0.1 mol% palladium (II) trifluoracetate [Pd(TFA)(2)] and 0.7 mol% 3.4,7,8-tetramethyl-1,10-phenanthroline (tm-phen) in DMF at 15 psig CO and 80 degrees C afforded indoles in good to excellent yields. When the reaction was conducted in toluene. the corresponding N-hydroxyindole was isolated. A mechanism that accounts for the formation of N-hydroxyindole is proposed. (c) 2005 Elsevier Ltd. All rights reserved.
Rapid and Efficient Synthesis of 1<i>H</i>-Indol-2-yl-1<i>H</i>-quinolin-2-ones
作者:Jeffrey T. Kuethe、Audrey Wong、Ian W. Davies
DOI:10.1021/ol035541i
日期:2003.10.1
A concise and efficient synthesis of the novel indol-2-yl-1H-quinolin-2-one ring system found in the potent and selective KDR kinase inhibitors 1-3 is presented.