1240100-09-7Relevant academic research and scientific papers
Indole-3-carbonitriles as DYRK1A inhibitors by fragment-based drug design
Meine, Rosanna,Becker, Walter,Falke, Hannes,Preu, Lutz,Loa?c, Nadège,Meijer, Laurent,Kunick, Conrad
, (2018/02/07)
Dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A) is a potential drug target because of its role in the development of Down syndrome and Alzheimer's disease. The selective DYRK1A inhibitor 10-iodo-11H-indolo[3, 2-c]quinoline-6-carboxy
Nickel-Catalyzed Cyanation of Aryl Chlorides and Triflates Using Butyronitrile: Merging Retro-hydrocyanation with Cross-Coupling
Yu, Peng,Morandi, Bill
supporting information, p. 15693 - 15697 (2017/12/02)
We describe a nickel-catalyzed cyanation reaction of aryl (pseudo)halides that employs butyronitrile as a cyanating reagent instead of highly toxic cyanide salts. A dual catalytic cycle merging retro-hydrocyanation and cross-coupling enables the conversion of a broad array of aryl chlorides and aryl/vinyl triflates into their corresponding nitriles. This new reaction provides a strategically distinct approach to the safe preparation of aryl cyanides, which are essential compounds in agrochemistry and medicinal chemistry.
Regiocontrolled Direct C?H Arylation of Indoles at the C4 and C5 Positions
Yang, Youqing,Gao, Pan,Zhao, Yue,Shi, Zhuangzhi
supporting information, p. 3966 - 3971 (2017/03/27)
An effective and practical strategy has been established for the direct and site-selective arylation of indoles at the C4 and C5 positions with the aid of a readily accessible, cheap, and removable pivaloyl directing group at the C3 position. This transfo
General and efficient synthesis of 2,3-unsubstituted indoles catalyzed by acidic mesoporous molecular sieves
Sun, Nan,Hong, Lingfen,Huang, Fang,Ren, Hong,Mo, Weimin,Hu, Baoxiang,Shen, Zhenlu,Hu, Xinquan
, p. 3927 - 3933 (2013/06/27)
A general and efficient method for the synthesis of 2,3-unsubstituted indoles has been established by the intramolecular cyclization of N-benzyl 2-anilinoacetals. Acidic mesoporous molecular sieve (MCM-41-SO3H) has shown excellent catalytic activity on this transformation, and the 2,3-unsubstituted indoles bearing 7-substituent or strong electron-withdrawing substituents also could be achieved by this protocol. Moreover, the heterogeneous catalyst, MCM-41-SO3H, could be conveniently recovered and reused without obvious loss of the catalytic activity. This work will provide an economic and environmental-benign method for the construction of various indole derivatives.
