反应详情

To a solution of (S)-tert-butyl 6-cyclopropyl-2-(5-(N-(1,1,1-trifluoropropan-2-yl)sulfamoyl)pyridin-2-yl)-1H-indole-1-carboxylate (503 mg, 0.99 mmol) and K2CO3 (276 mg, 2 mmol) in DMF (5 mL) was added allyl bromide (0.11 mL, 1.30 mmol). The mixture was stirred at room temperature for 2 hrs, and quenched with water (60 mL). The mixture was extracted with CH2Cl2 (3×20 mL). The solvent was then evaporated and (S)-tert-butyl 2-(5-(N-allyl-N-(1,1,1-trifluoropropan-2-yl)sulfamoyl)pyridin-2-yl)-6-cyclopropyl-1H-indole-1-carboxylate was obtained as a light yellow oil (500 mg, 92% yield). MS m/z 550.3 M+H+. This material was used in the next step without further purification.

1. customquenched with water (60 mL)
2. extractionThe mixture was extracted with CH2Cl2 (3×20 mL)
3. customThe solvent was then evaporated