- Access to 2-pyridinylamide and imidazopyridine from 2-fluoropyridine and amidine hydrochloride
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Under catalyst-free conditions, an efficient method to synthesize 2-pyridinylamides has been developed, and the protocol uses inexpensive and readily available 2-fluoropyridine and amidine derivatives as the starting materials. Simultaneously, the copper-catalysed approach to imidazopyridine derivatives has been established with high chemoselectivity and regiospecificity. The results suggest that the nitrogen-heterocycles containing iodide substituents can also be compatible for the reaction via the cascade Ullmann-type coupling, and the nucleophilic substitution reaction provides the target products in a one-pot manner.
- Chen, Lu,Huang, Shuo,Ji, Xiaoliang,Li, Jiaming,Li, Jian,Li, Yibiao,Liu, Jiasheng,Peng, Shiyong,Zhang, Kun
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supporting information
p. 9292 - 9299
(2020/12/03)
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- KIF18A INHIBITORS
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Compounds of formula (I): (I), as defined herein, and synthetic intermediates thereof, which are capable of modulating KIF18A protein thereby influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of KIF18A.
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Paragraph 0336
(2020/07/14)
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- Condensation of substituted 2-aminopyridine with β-ketocarboxylic esters: 4H-pyrido[1,2-a]pyrimidin-4-ones and pyridin-2-ones
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We report the condensation of substituted 2-aminopyridines 5 with β- ketocarboxylic esters in polyphosphoric acid. In this reaction were obtained together with the target compounds, 4H-pyrido[1,2-a]pyrimidin-4-ones 6 also the pyridin-2-ones 7. All the compounds 7 were tested for their calcium- antagonistic activity but failed to evoke any vasorelaxant response.
- Ferrarini, Pier Luigi,Mori, Claudio,Manera, Clementina,Mori, Filippo,Calderone, Vincenzo,Martinotti, Enrica
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p. 1123 - 1127
(2007/10/03)
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