- Pd-Catalyzed Dearomatization of Indole Derivatives via Intermolecular Heck Reactions?
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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.
- Yang, Ping,Xu, Ren-Qi,Zheng, Chao,You, Shu-Li
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supporting information
p. 235 - 241
(2020/01/28)
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- Indoline derivatives a series of structure containing asymmetric squaraine cyanine small molecule and its application
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The invention provides a series of novel asymmetric squarine micromolecules, and an application thereof. By introducing different electricity-rich aromatic units in two ends of a squaric acid four-membered ring as donor units, a series of low narrow-gap asymmetric squarine micromolecule photovoltaic materials are designed and synthesized. The series of the low narrow-gap asymmetric squarine micromolecule photovoltaic materials have strong absorption in visible and near-infrared light regions; absorption spectra cover400-900 nm; and HOMO and LUMO of the series of the low narrow-gap asymmetric squarine micromolecule photovoltaic materials can match well with energy levels of an acceptor material PCBM to obtain a high open-circuit voltage. The compounds have good solubility and film-forming property, so that the compounds can be applied in bulk hetero-junction organic solar cells processed by low-cost solution. Performances of the organic solar cells with asymmetric squaric acid macromolecules as donor materials can reach an open-circuit voltage Voc=0.72-1.05 V, a short-circuit current Jsc=8.80-12.67 mA/cm, a fill factor (FF)=0.38-0.55, and photoelectric conversion efficiency (PCE)=2.41-6.10%.
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Paragraph 0194-0197
(2019/02/02)
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- Indole derivatives process for their preparation, pharmaceutical compositions containing them and their medicinal application
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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.
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Page/Page column 18
(2010/02/05)
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