- High-selectivity fibroblast growth factor receptor inhibitor and application
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The invention discloses a high-selectivity fibroblast growth factor receptor inhibitor and application, and particularly relates to a compound shown in a formula (I) or a pharmaceutically acceptable salt, a solvate, a geometric isomer, a stereoisomer, a tautomer and any mixture thereof. The compound shown in the formula (I) or the pharmaceutically acceptable salt, the solvate and the pharmaceutical composition thereof can be applied to prevention or treatment of diseases related to FGFR4 activity or overexpression, and can also be combined with other medicines to be used for treating various related diseases, especially for treating various cancers, wherein the cancers may be liver cancer, lung cancer, gastric cancer, breast cancer, ovarian cancer, prostate cancer, renal cell carcinoma, skin cancer, colon cancer, bile duct cancer, glioma or sarcoma.
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- Facile synthesis of 1,3,4-oxadiazoles via iodine promoted oxidative annulation of methyl-azaheteroarenes and hydrazides
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An oxidative sp3 C–H bond of methyl-azaheteroarenes protocol was reported for the synthesis of 1,3,4-oxadiazoles via [4 + 1] annulation with hydrazides. This protocol enables 1,3,4-oxadiazole and quinoline linked diheterocycles via selective oxidation of sp3 C–H bond of methyl-azaheteroarenes in the presence of I2-DMSO. The reaction has a broad substrate scope and good functional group tolerance for methyl-azaheteroarenes and hydrazides.
- Shang, Zhi-Hao,Sun, Ji-Na,Guo, Jiang-Shan,Sun, Yuan-Yuan,Weng, Wei-Zhao,Zhang, Zhen-Xiao,Li, Zeng-Jing,Zhu, Yan-Ping
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supporting information
(2020/01/08)
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- N-Heterocyclic Carbene Copper(I) Complex Catalyzed Coupling of (Hetero)aryl Chlorides and Nitrogen Heterocycles: Highly Efficient Catalytic System
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A highly efficient catalytic system for the N-arylation reactions of (hetero)aryl chlorides and nitrogen heterocycles with a copper(I) complex containing a 1,10-phenanthroline analogue N-heterocyclic carbene (NHC) has been reported. The complex was characterized by 1H NMR and 13C NMR spectroscopy and elemental analysis, and its structure was determined by single-crystal X-ray diffraction. The NHC-copper(I) complex was employed as pre-catalyst for Ullmann type N-arylation reactions of (hetero)aryl chlorides with various azoles. A variety of hindered and functionalized azoles and (hetero)aryl chlorides were transformed in good to excellent yields.
- Zhang, Mengyao,Zhang, Yingying,Zhang, Huixin,Zeng, Yongfei,Liu, Guiyan
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p. 1252 - 1256
(2020/08/05)
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- Double Dehydrogenation of Primary Amines to Nitriles by a Ruthenium Complex Featuring Pyrazole Functionality
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A ruthenium(II) complex bearing a naphthyridine-functionalized pyrazole ligand catalyzes oxidant-free and acceptorless selective double dehydrogenation of primary amines to nitriles at moderate temperature. The role of the proton-responsive entity on the ligand scaffold is demonstrated by control experiments, including the use of a N-methylated pyrazole analogue. DFT calculations reveal intricate hydride and proton transfers to achieve the overall elimination of 2 equiv of H2.
- Dutta, Indranil,Yadav, Sudhir,Sarbajna, Abir,De, Subhabrata,H?lscher, Markus,Leitner, Walter,Bera, Jitendra K.
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p. 8662 - 8666
(2018/07/09)
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- GLYCOSIDASE INHIBITORS
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Compounds of formula (I) wherein A, R, W, Q, n and m have the meaning according to the claims can be employed, inter alia, for the treatment of tauopathies and Alzheimer's disease.
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- GLYCOSIDASE INHIBITORS
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Compounds of formula (I) wherein A, R, W, Q, n and m have the meaning according to the claims can be employed, inter alia, for the treatment of tauopathies and Alzheimer's disease.
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- Highly active palladium catalysts containing a 1,10-phenanthroline analogue N-heterocyclic carbene for room temperature Suzuki-Miyaura coupling reactions of aryl chlorides with arylboronic acids in aqueous media
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Two new palladium (II) complexes containing a 1,10-phenanthroline analogue N-heterocyclic carbene (NHC) have been synthesized. The complexes were characterized by 1H and 13C NMR spectroscopy and elemental analysis and their structures were determined by single-crystal X-ray diffraction. The NHC-palladium complexes were employed as catalysts for Suzuki-Miyaura coupling reactions of aryl chlorides with arylboronic acids in aqueous media at room temperature. The cross-coupling reactions were highly efficient with low catalysts loadings.
- Liu, Guiyan,Liu, Chengxin,Han, Fangwai,Wang, Zhongliang,Wang, Jianhui
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supporting information
p. 726 - 731
(2017/03/31)
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- 1. 8 - naphthyridine binuclear copper (I) complexes, preparation method and application
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The invention discloses a 1,8-naphthyridine binuclear copper (I) complex with a molecular formula shown in the specification. The complex is the first naphthyridine binuclear copper complex with a DNA cutting function discovered so far, and can be used for pyrolysis of DNA by virtue of a hydrolysis mechanism under the condition that oxygen and a reducing agent are not used to ensure that the complex can be possibly used as a new antitumor medicament in the field of medicament research and development. The invention also discloses a preparation method of the 1,8-naphthyridine binuclear copper (I) complex. The invention also discloses an application of the 1,8-naphthyridine binuclear copper (I) complex which can be used for cutting DNA.
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Paragraph 0059; 0060
(2017/06/13)
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- Olefin oxygenation by water on an iridium center
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Oxygenation of 1,5-cyclooctadiene (COD) is achieved on an iridium center using water as a reagent. A hydrogen-bonding interaction with an unbound nitrogen atom of the naphthyridine-based ligand architecture promotes nucleophilic attack of water to the met
- Ghatak, Tapas,Sarkar, Mithun,Dinda, Shrabani,Dutta, Indranil,Rahaman, S. M. Wahidur,Bera, Jitendra K.
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p. 6168 - 6171
(2015/06/02)
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- Synthesis of 1,8-naphthyridine and BF2-based isomers and their application in fluorogenic sensing Cd2+
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A series of isomers were synthesized and identified, two isomers of which were developed as the dual-channel fluorescent probe toward Cd2+. BF2 dissociates from the probe upon reaction with CdCl2, demonstrating a new approach for sensing Cd2+.
- Liu, Xingjiang,Chen, Mingxing,Liu, Ziping,Yu, Mingming,Wei, Liuhe,Li, Zhanxian
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p. 658 - 663
(2014/02/14)
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- HETEROARYL COMPOUNDS AND METHODS OF USE THEREOF
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Provided herein are heteroaryl compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. In one embodiment, the compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as CNS disorders and metabolic disorders, including, but not limited to, e.g., neurological disorders, psychosis, schizophrenia, obesity, and diabetes
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Page/Page column 127
(2011/12/14)
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- Substituted arylamides
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Substituted benzamide compounds are provided along with methods for the use of those compounds for treating cancer.
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Page/Page column 34
(2010/10/20)
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