反应详情

To a suspension of 540 mg (2.82 mmol) of 6-amino-5-methyl-1H-indazole-7-carboxylic acid in 20 mL of anhydrous acetonitrile is added 771 mg (2.82 mmol) of 2-(3-chloro-pyridin-2-yl)-5-difluoromethyl-2H-pyrazole-3-carboxylic acid followed by 1.02 mL (12.7 mmol) of pyridine. The mixture is stirred at ambient temperature during 30 minutes. Then the suspension is cooled to 0° C. and 766 μL (9.9 mmol) of methanesulfonyl chloride is added dropwise. The mixture is stirred at 50° C. for 16 hours. Then the solvent is evaporated and the residue is triturated with a minimum of cold water. The precipitate, which is formed is filtrated, washed with cold water and dried. The pale yellowish product obtained is engaged in the next step; LC/MS:429/431 (M+H)+.

1. temperatureThen the suspension is cooled to 0° C.
2. stirringThe mixture is stirred at 50° C. for 16 hours
3. customThen the solvent is evaporated
4. customthe residue is triturated with a minimum of cold water
5. customThe precipitate, which is formed
6. filtrationis filtrated
7. washwashed with cold water
8. customdried
9. customThe pale yellowish product obtained