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温度

0 °C

Borane dimethyl sulfide complex (2M in THF, 26.3 mL) was added dropwise over 10 minutes to a solution of 2-(3-(bromomethyl)-5-fluorophenyl)acetic acid [Aromatic Intermediate 4, step a] (6.5 g) in THF (120 mL) at 0° C. The mixture was stirred at 0° C. for 10 minutes and then at 20° C. for 1 hour. The reaction mixture was quenched by dropwise addition of methanol and the solvents were removed under reduced pressure. The crude product was purified by flash silica chromatography using 30% ethyl acetate in isohexane. Fractions containing the product were concentrated to dryness to afford the titled compound. Yield 4.70 g.

1. waitat 20° C. for 1 hour
2. customThe reaction mixture was quenched by dropwise addition of methanol
3. customthe solvents were removed under reduced pressure
4. customThe crude product was purified by flash silica chromatography
5. additionFractions containing the product
6. concentrationwere concentrated to dryness