1227594-82-2Relevant articles and documents
Preparation method of 2-trifluoromethyl-3-fluoro-4-picolinic acid and derivatives thereof
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Paragraph 0038-0042; 0043; 0048-0051; 0057-0061, (2020/04/17)
The invention discloses a preparation method of 2-trifluoromethyl-3-fluoro-4-picolinic acid and derivatives thereof, and is characterized in that provided is the preparation method of 2-trifluoromethyl-3-fluoro-4-picolinic acid and the derivatives thereof by a method of introducing trifluoromethyl into 2-site of a polysubstituted pyridine ring through a free radical mechanism, wherein the preparation method is suitable for large-scale application. The method for directly carrying out trifluoromethylation reaction on the 2-site of 3-fluoro-4-pyridine carboxylic acid alkyl ester is reported forthe first time, and is simple and convenient in process, easily available in raw materials, high in conversion rate and simple in reaction post-treatment operation. Meanwhile, the selectivity of the method in introducing trifluoromethyl into the 2-site of pyridine is quite high, and a single product with trifluoromethyl substituted at the 2-site can be obtained only through simple recrystallization.
SUBSTITUTED 5,6,7,8-TETRAHYDRO[1,2,4]TRIAZOLO[4,3-A]PYRIDINE-3(2H)-ONES AND 2,5,6,7-TETRAHYDRO-3H-PYRROLO[2,1-C][1,2,4]TRIAZOL-3-ONES, AND USE THEREOF
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Paragraph 0756-0758, (2019/06/12)
The present application relates to novel substituted 5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-3(2H)-ones and 2,5,6,7-tetrahydro-3H-pyrrolo[2,1-c][1,2,4]triazol-3-ones, to processes for preparation thereof, to the use thereof, alone or in combinations, for treatment and/or prophylaxis of diseases, and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially for treatment and/or prophylaxis of lung inflammation disorders.