- Synthetic method of 4-fluoroindazole 3-carbonitrile or derivative thereof
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The invention is applicable to the technical field of chemical synthesis, and provides a synthesis method of 4-fluoroindazole 3-carbonitrile or derivatives thereof, which comprises the following steps: reacting 2-fluoro-6-nitrophenylacetaldehyde, ethanol, sodium bicarbonate, hydroxylamine hydrochloride and water to obtain 2-fluoro-6-nitrophenylethyloxime; reacting 2-fluoro-6-nitroacetoxime with acetic anhydride to obtain 2-fluoro-6-nitrophenylacetonitrile; reacting 2-fluoro-6-nitrophenylacetonitrile, tetrahydrofuran, methanol, water, ammonium chloride and iron powder, and reacting with glacialacetic acid and acetic anhydride to obtain 2-acetylamino-6-fluorophenylacetonitrile; reacting 2-acetylamino-6-fluorophenylacetonitrile, glacial acetic acid, acetic anhydride and isoamyl nitrite, andreacting with ethanol and sodium hydroxide to obtain the 4-fluoroindazole 3-carbonitrile. The synthesis method provided by the invention is mild in reaction condition and easy to operate, and the adopted raw materials are conventional and harmless.
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Paragraph 0036; 0040; 0044; 0045; 0049
(2020/12/10)
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- Structure-based design of potent and selective inhibitors of the metabolic kinase PFKFB3
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A weak screening hit with suboptimal physicochemical properties was optimized against PFKFB3 kinase using critical structure-guided insights. The resulting compounds demonstrated high selectivity over related PFKFB isoforms and modulation of the target in
- Boyd, Scott,Brookfield, Joanna L.,Critchlow, Susan E.,Cumming, Iain A.,Curtis, Nicola J.,Debreczeni, Judit,Degorce, Sébastien L.,Donald, Craig,Evans, Nicola J.,Groombridge, Sam,Hopcroft, Philip,Jones, Neil P.,Kettle, Jason G.,Lamont, Scott,Lewis, Hilary J.,MacFaull, Philip,McLoughlin, Sheila B.,Rigoreau, Laurent J. M.,Smith, James M.,St-Gallay, Steve,Stock, Julie K.,Turnbull, Andrew P.,Wheatley, Edward R.,Winter, Jon,Wingfield, Jonathan
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p. 3611 - 3625
(2015/05/05)
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- N1-PYRAZOLOSPIROKETONE ACETYL-COA CARBOXYLASE INHIBITORS
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The invention provides a compound of Formula (I) or a pharmaceutically acceptable salt of the compound, wherein R1, R2, R3 and R4 are as described herein; pharmaceutical compositions there-of; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl- CoA carboxylase enzyme(s) in an animal
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- N2-PYRAZOLOSPIROKETONE ACETYL-COA CARBOXYLASE INHIBITORS
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The invention provides a compound of Formula (I) or a pharmaceutically acceptable salt of said compound, wherein R1, R2, R3 and R4 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl- CoA carboxylase enzyme(s) in an animal.
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