- Ru(III)-catalyzed construction of variously substituted quinolines from 2-aminoaromatic aldehydes (ketones) and isoxazoles: Isoxazoles as cyclization reagent and cyano sources
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A Ru(Ⅲ)-catalyzed annulation reaction of 2-aminoaromatic aldehydes (ketones) and isoxazoles to afford diverse 3-cyanoquinolines has been developed. Notably, isoxazole acted as a cyclization reagent and nontoxic cyano source via N-O bond cleavage and fragm
- Cui, Xiuling,Han, Xiliang,Hu, Di,Hu, Wei,Pi, Chao,Wu, Yangjie
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supporting information
(2022/01/28)
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- 3-nitrile quinoline derivative and preparation method thereof
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The invention discloses a 3-nitrile quinoline derivative. The structural formula of the 3-nitrile quinoline derivative is shown as a formula I, wherein R1 is hydrogen, alkyl or aryl; R2-R5 are respectively and independently hydrogen, halogen, alkyl, alkoxy, trifluoromethyl, ester group, hydroxyl or amino; and R6 is hydrogen, alkyl, ester group, aryl or substituted aryl. According to the 3-nitrile quinoline derivative provided by the invention, R1-R6 sites can be connected with various substituent groups, and the 3-nitrile quinoline derivative is an organic synthesis intermediate with wide application and has important application value in the fields of medicines and organic synthesis. The invention further provides the preparation method of the 3-nitrile quinoline derivative, the preparation method can be carried out under the air condition, the reaction condition is mild and easy to control, the used raw materials are easy to obtain, toxic nitrile compounds are not needed to serve as nitrile groups sources, the substrate application range is wide, the reaction conversion rate is high, high selectivity and yield can be obtained within short time, and the method is simple in post-treatment, green, environment-friendly and suitable for large-scale industrial production.
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Paragraph 0082-0084
(2021/11/10)
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- FATTY ACID SYNTHASE INHIBITORS
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This invention relates to novel spirocyclic piperidines according to Formula (I) which are inhibitors of fatty acid synthase (FAS), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the treatment of cancers.
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Page/Page column 73
(2014/01/18)
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- FATTY ACID SYNTHASE INHIBITORS
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Disclosed are compounds having Formula (I), or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R5, R6, R7, R8, R8a, R9 Y, and m are defined herein and methods of using the same.
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Page/Page column 49; 50; 65
(2013/04/24)
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- FATTY ACID SYNTHASE INHIBITORS
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This invention relates to spirocyclic piperidines according to Formula (I) and the use of spirocyclic piperidines for the modulation, notably the inhibition of the activity or function of fatty acid synthase (FAS). Suitably, the present invention relates to the use of spirocyclic piperidines in the treatment of cancer.
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Page/Page column 119-120
(2013/03/26)
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- FATTY ACID SYNTHASE INHIBITORS
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Disclosed are compounds having Formula (I), wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, Y, m, and n are defined herein and methods of using the same.
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Page/Page column 61
(2014/01/07)
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