反应详情

Methyl[1-(4-cyanophenyl)-7-methoxy-3-methyl-3H-pyrazolo[3,4-c]quinolin-8-yloxy]-(4-fluorophenyl)acetate (260 mg, 524 μmol) is dissolved in tetrahydrofuran and methanol (66 ml each). Sodium hydroxide solution (1.0 M, 1.58 ml, 1.58 mmol) is subsequently added dropwise. The reaction mixture is stirred at room temperature for 18 h. When the reaction is complete, the mixture is evaporated to dryness in vacuo, and the residue obtained is taken up in water (100 ml). The mixture is carefully acidified to pH 5 by addition of hydrochloric acid (1.0 M) and stirred for a further 30 min. The precipitate formed is filtered off with suction and rinsed with water. The filter cake is subsequently suspended in 2-propanol (5 ml), filtered off with suction again, and the residue is dried overnight in a high vacuum, giving [1-(4-cyanophenyl)-7-methoxy-3-methyl-3H-pyrazolo[3,4-c]quinolin-8-yl-oxy]-(4-fluorophenyl)acetic acid (235 mg, 488 μmol) as a solid having a melting point of 211.6° C. MS: 483.1 (M+H+), TLC (HPTLC): Rf=0.11 (ethanol).

1. customthe mixture is evaporated to dryness in vacuo
2. customthe residue obtained
3. stirringstirred for a further 30 min
4. customThe precipitate formed
5. filtrationis filtered off with suction
6. washrinsed with water
7. filtrationfiltered off with suction again
8. customthe residue is dried overnight in a high vacuum