- BTK Inhibitors and uses thereof
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The invention discloses a bruton's tyrosine kinase (BTK) inhibitor and use thereof. Specifically, the invention provides heteroaromatic compounds or stereoisomers, geometrical isomers, tautomers, racemates, nitrogen oxides, hydrates, solvates, metabolites and pharmaceutically acceptable salts or prodrugs thereof, and pharmaceutical compositions containing the heteroaromatic compounds; the invention also discloses use of the heteroaromatic compounds or the pharmaceutical compositions containing the heteroaromatic compounds in preparation of medicines; the medicines can be used for treating autoimmune diseases, inflammatory diseases or proliferative diseases.
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Paragraph 1771; 1780-1782
(2020/05/02)
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- Synthesis of 2,3-dihydro-1H-pyrrolo[1,2-a]benzimidazoles via the cyclopropyliminium rearrangement of substituted 2-cyclopropylbenzimidazoles
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2-Cyclopropylbenzimidazole derivatives with various substituents in the small ring undergo cyclopropyliminium rearrangement into 2,3- dihydropyrrolobenzimidazoles substituted at positions 1, 2 or 3. The substrates containing a functional group in position 1 of the cyclopropane ring form products substituted at position 3. Substituents at position 2 in most cases lead to the formation of a mixture of isomers. The reaction can be directed to yield one of the isomers predominantly by varying the solvent polarity.
- Salikov, Rinat F.,Platonov, Dmitry N.,Frumkin, Aleksandr E.,Lipilin, Dmitry L.,Tomilov, Yury V.
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supporting information
p. 3495 - 3505
(2013/04/23)
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- Synthesis, crystal structure and biological activity of 1-cyano-N-phenylcyclopropanecarboxamide
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A cyclopropane derivative, 1-cyano-N-phenylcyclopropanecarboxamide (C 11H10N2O) was synthesized and its structure was studied by X-ray diffraction, FTIR, 1H NMR spectrum and MS. The crystals are monoclinic, space group Pbc
- Xue, Yong-Lai,Liu, Xing-Hai,Zhang, Yong-Gang
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experimental part
p. 1571 - 1574
(2012/09/07)
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- Synthesis, crystal structure and biological activity of 1-Cyano-N-(2,4-dichlorophenyl)cyclopropanecarboxamide
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A cyclopropane derivative, 1-cyano-N-(2,4-dichlorophenyl) cyclopropanecarboxamide (C11H8N2OCl2) was synthesized and its structure was studied by X-ray diffraction, FTIR, 1H NMR, MS and elemental analysis. The crystals are monoclinic, space group C2 with a
- Xue, Yong-Lai,Zhang, Yong-Gang,Liu, Xing-Hai
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experimental part
p. 5087 - 5089
(2012/10/08)
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- Synthesis, crystal structure and biological activity of 1-Cyano-N-(4-bromophenyl)cyclopropanecarboxamide
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A cyclopropane derivative, 1-cyano-N-(4-bromophenyl)cyclopropanecarboxamide (C11H9N2OBr) was synthesized and its structure was studied by X-ray diffraction, FTIR, 1H NMR spectrum and MS. The crystal is triclinic, space group P-1 with α = 8.902(4), β = 10.
- Xue, Yong-Lai,Zhang, Yong-Gang,Liu, Xing-Hai
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experimental part
p. 3016 - 3018
(2012/08/29)
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- Synthesis, bioactivity, theoretical and molecular docking study of 1-cyano-N-substituted-cyclopropanecarboxamide as ketol-acid reductoisomerase inhibitor
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Ketol-acid reductoisomerase (KARI; EC 1.1.1.86) catalyzes the second common step in branched-chain amino acid biosynthesis. The catalyzed process consists of two stages, the first of which is an alkyl migration from one carbon atom to its neighbouring ato
- Liu, Xing-Hai,Chen, Pei-Quan,Wang, Bao-Lei,Li, Yong-Hong,Wang, Su-Hua,Li, Zheng-Ming
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p. 3784 - 3788
(2008/02/08)
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- Reaction of cyclopropane carboxylic acid derivatives with sulphur tetrafluoride - An example of a diastereoselective ring opening
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Cyclopropane carboxylic acid derivatives can be converted into trifluoromethyl group-containing compounds using SF4. In the case of a bicyclic cyclopropane carboxylic acid lactone, similar treatment with sulphur tetrafluoride resulted in the cyclopropane ring opening in a diastereoselective manner.
- Hell,Finta,Dmowski,Faigl,Pustovit,Toke,Harmat
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p. 297 - 301
(2007/10/03)
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- Preparation and Cleavage of Some Cyclopropane Derivatives
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Alkylation of active methylene compounds with 1,2-dibromoethane using anhyd.K2CO3/DMF at room temperature gives cyclopropane derivatives which undergo selective transformation by simple methods.Cyclopropanes, obtained by the condensation of α-diazoacetophenones with olefins, are cleaved to trisubstituted olefins with Grignard reagent.Hydration of the products has also been studied.
- Podder, Ranjan Kumar,Sarkar, Ranjit Kumar,Ray, Suvas C.
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p. 530 - 536
(2007/10/02)
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