反应详情

温度

80 °C

(4-(Trifluoromethoxy)phenyl)hydrazine hydrochloride (1 equiv.) is taken in 7% sulfuric acid in 1,4-dioxane. 1-Methylpiperidin-4-one hydrochloride (0.76-1.4 equiv.) is added and the mixture is stirred at 80° C. for 6 h. The reaction is monitored by TLC and LCMS. After completion of the reaction, the reaction mixture is concentrated, then slowly quenched with aq. NaHCO3 solution and extracted with EtOAc. The organic layer is dried over anhydrous sodium sulfate, evaporated to dryness and purified by column chromatography to afford 2-methyl-8-(trifluoromethoxy)-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole.

1. customAfter completion of the reaction
2. concentrationthe reaction mixture is concentrated
3. customslowly quenched with aq. NaHCO3 solution
4. extractionextracted with EtOAc
5. dry with materialThe organic layer is dried over anhydrous sodium sulfate
6. customevaporated to dryness
7. custompurified by column chromatography