反应详情

60% NaH (84 mg, 2.1 mmol) is added to a solution of 2-(5-bromo-pyridin-3-yl)-1H-indole (192 mg, 0.70 mmol) in THF (20 mL) and the temperature is kept below 0° C. After the addition, the mixture is stirred at room temperature for 30 min. MeI (125 mg, 0.88 mmol) is added to the mixture at 0° C. and the mixture is stirred at room temperature for 3 hrs. Then the solvent is removed and the residue is dissolved in EtOAc and washed with water. The organic layer is separated, dried and concentrated. The crude product is purified by flash column chromatography to give 173 mg of 2-(5-bromo-pyridin-3-yl)-1-methyl-1H-indole.

1. customis kept below 0° C
2. additionAfter the addition
3. stirringthe mixture is stirred at room temperature for 3 hrs
4. customThen the solvent is removed
5. dissolutionthe residue is dissolved in EtOAc
6. washwashed with water
7. customThe organic layer is separated
8. customdried
9. concentrationconcentrated
10. customThe crude product is purified by flash column chromatography