反应详情

Diethylamine (0.48 mL, 4.63 mmol, 3 eq) was added into the crude 5-(2-Methanesulfonyloxy-ethyl)-2-trifluoromethyl-1H-indole-3-carboxylic acid benzyl ester in dioxanes (20 mL) solution. The reaction mixture was heated to reflux overnight. After the solvent was removed, the residue was purified by gravity chromatography (SiO2, ethyl acetate-methanol-NH4OH) to yield the desire indole amine as pale yellow gel (20.0% yield). Elemental Analysis: C23H25F3N2O2.HCl: Calcd: C: 60.73; H: 5.76; N: 6.16. Found: C: 60.40; H: 5.83; N: 6.06. ESI-MS: m/z 419.73 (M+H)+.

1. temperatureThe reaction mixture was heated
2. temperatureto reflux overnight
3. customAfter the solvent was removed
4. customthe residue was purified by gravity chromatography (SiO2, ethyl acetate-methanol-NH4OH)