327021-84-1Relevant articles and documents
Pd-Catalyzed Dearomatization of Indole Derivatives via Intermolecular Heck Reactions?
Yang, Ping,Xu, Ren-Qi,Zheng, Chao,You, Shu-Li
supporting information, p. 235 - 241 (2020/01/28)
Pd-catalyzed intermolecular dearomative Heck reaction of indoles with aryl iodides is described. The challenges on both reactivity and regioselectivity are addressed by the judicious regulation of the geometric and electronic properties of the substrates. An array of indoline derivatives bearing C2-quaternary center is obtained in good to excellent yields (up to 93%) with exclusive regioselectivity under operationally simple conditions. The mechanistic proposal is supported by detailed DFT calculations.
Indole derivatives process for their preparation, pharmaceutical compositions containing them and their medicinal application
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Page/Page column 18, (2010/02/05)
A chemical compound of formula (I) wherein: R1and R2are independently selected from hydrogen and alkyl; R3is alkyl; R4, R6and R7are independently selected from hydrogen, halogen, hydroxy, alkyl, aryl, amino, alkylamino, dialkylamino, alkoxy, aryloxy, alkylthio, alkylsufoxyl, alkylsulfonyl, nitro, carbonitrile, carbo-alkoxy, carbo-aryloxy and carboxyl; R5is selected from hydrogen, halogen, hydroxy, alkyl, aryl, amino, alkylamino, dialkylamino, alkoxy, aryloxy, alkylthio, alkylsulfoxyl, alkylsulfonyl, nitro, carbonitrile, carbo-alkoxy, carbo-aryloxy and carboxyl; A is a 5- or 6-membered partially unsaturated or aromatic heterocyclic ring or a 5- or 6-membered partially unsaturated carbocyclic ring, wherein if A is a 6-membered partially unsaturated carbocyclic ring then at least one of R4to R7is other than hydrogen, and pharmaceutically acceptable salts, addition compounds and prodrugs thereof, and the use thereof in therapy, particularly as an agonist or antagonist of a 5HT receptor, particularly a 5HT2Creceptor, for instance in the treatment of disorders of the central nervous system; damage to the central nervous system; cardiovascular disorders; gastrointestinial disorders; diabetes insipidus, and sleep apnea, and particularly for the treatment of obesity.