反应详情

温度

0 °C

To a solution of 2-(5-methoxy-1-methyl-1H-indol-3-yl)-1-(toluene-4-sulfonyl)-1H-pyrrolo[2,3-b]pyridine [24.5 g, Reference Example 13(b)] in dichloromethane (500 mL), at 0° C. under an atmosphere of nitrogen, was added a solution of boron tribromide in dichloromethane (60 mL, 1.0M) and the mixture was stirred at 0° C. for 1 hour. The reaction mixture was allowed to warm slowly to ambient temperature and stirring continued for 12 hours. A solution of sodium carbonate (1M, 250 mL) was added to the mixture and stirring was continued vigorously for 3 hours. The precipitated solid was collected by filtration, washed with dichloromethane (100 mL) and dried to give the title compound (18.75 g) as a colourless solid, m.p. 256-257° C. MS: 418 (MH+).

1. temperatureto warm slowly to ambient temperature
2. stirringstirring
3. waitcontinued for 12 hours
4. stirringstirring
5. waitwas continued vigorously for 3 hours
6. filtrationThe precipitated solid was collected by filtration
7. washwashed with dichloromethane (100 mL)
8. customdried