反应详情

To a suspension, stirred at 20° C., of 2 g (6.96 mmol) of 5-fluoro-1-[(3-fluorophenyl)-methyl]-1H-indole-2-carboxylic acid, prepared in step 1.1, in 80 mL of dry toluene are added 5.08 mL (69.62 mmol) of thionyl chloride. The reaction mixture is stirred for 2 hours at reflux and is then concentrated under reduced pressure. The resulting product is taken up in 10 mL of dichloromethane, and this solution is poured dropwise into a solution of 9.12 mL (69.62 mmol) of 30% aqueous ammonia. The reaction mixture is stirred for 14 hours at 20° C. After this time, a solid is collected by filtration, and is triturated in 50 mL of diisopropyl ether. After filtering off and drying under reduced pressure, 0.58 g of the expected product is collected.

1. temperatureat reflux
2. concentrationis then concentrated under reduced pressure
3. stirringThe reaction mixture is stirred for 14 hours at 20° C
4. filtrationAfter this time, a solid is collected by filtration
5. customis triturated in 50 mL of diisopropyl ether
6. filtrationAfter filtering off
7. dry with materialdrying under reduced pressure, 0.58 g of the expected product
8. customis collected