2-Iodoxybenzoic acid → 2-(3-Fluoro-4-methoxy-phenyl)-cyclopropanecarbaldehyde
反応式
[F:1][C:2]1[CH:3]=[C:4]([CH:10]2[CH2:12][CH:11]2[CH2:13][OH:14])[CH:5]=[CH:6][C:7]=1[O:8][CH3:9].I(C1C=CC=CC=1C(O)=O)(=O)=O>CS(C)=O>[F:1][C:2]1[CH:3]=[C:4]([CH:10]2[CH2:12][CH:11]2[CH:13]=[O:14])[CH:5]=[CH:6][C:7]=1[O:8][CH3:9]参加物
4
反応条件
- 温度
- 0 °C
実験手順
After [2-(3-fluoro-4-methoxy-phenyl)-cyclopropyl]-methanol (0.30 g, 1.52 mmol) obtained in Step A was dissolved in DMSO (5 mL), 2-iodoxybenzoic acid (1.248 g, 4.58 mmol) was added thereto at 0° C., and the mixture was stirred at room temperature for 3 hours. After the termination of the reaction, the reactant was concentrated under reduced pressure, added with water, and then extracted with EtOAc. The organic layer was separated, dried with MgSO4, concentrated under reduced pressure, and then purified by column chromatography (eluent, EtOAc/Hex=1/3) to obtain the title compound (0.265 g, 89%).