反应详情

温度

80 °C

N1-cyclopropyl-5-((2-amino-4-pyridyl)oxy)-1H-1-indolecarboxamide (400 mg, CAS No. 417722-12-4) described in WO02/32872, 2-chloroethyl isocyanate (150 mg) and tetrahydrofuran (5 ml) were stirred at 80° C. for 1.5 hours. The mixture was cooled to room temperature, silica gel was added, and the solvent was distilled off under reduced pressure. The silica gel was charged into a dry column packed with silica gel, and purification was performed by column chromatography (hexane:ethyl acetate=1:1, followed by ethyl acetate) to yield 280 mg of a colorless powder.

1. temperatureThe mixture was cooled to room temperature
2. additionsilica gel was added
3. distillationthe solvent was distilled off under reduced pressure
4. additionThe silica gel was charged into a dry column
5. custompacked with silica gel, and purification