反应详情

To a suspension of 400 mg (1.89 mmol) of 6-amino-5-chloro-1H-indazole-7-carboxylic acid in 16 mL of anhydrous tetrahydrofuran is added 479 mg (1.89 mmol) of 2-(3-chloro-pyridin-2-yl)-5-methoxy-2H-pyrazole-3-carboxylic acid followed by 684 μL (8.50 mmol) of pyridine. The mixture is stirred at ambient temperature during 30 minutes. Then the suspension is cooled to 0° C. and 516 μL (6.66 mmol) of methanesulfonyl chloride are added dropwise. The mixture is stirred at ambient temperature for 5 hours. Then the solvent is evaporated and the residue is triturated with a minimum of cold water. The precipitate, which is formed is filtrated and washed with cold water. The pale yellowish product obtained (870 mg) is engaged in the next step; LC/MS:530/532 (M+H)+.

1. temperatureThen the suspension is cooled to 0° C.
2. stirringThe mixture is stirred at ambient temperature for 5 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. customThe pale yellowish product obtained (870 mg)