反应详情

温度

90 °C

Morpholine (73.5 μL), cetyltrimethylammoniumbromide (14.6 mg), bis(tri-tert-butylphosphine)palladium(0) (41 mg) and 50% aqueous solution of sodium hydroxide (96 μL) were added to a solution of tert-butyl {[4-bromo-1-(3-methoxypropyl)-1H-indol-3-yl]methy}cyclopropylcarbamate (205 mg) in toluene (3 ml) and the mixture was stirred under argon atmosphere at 90° C. for 23 hours. The reaction mixture was cooled to room temperature, diluted with water and extracted with ethyl acetate. The obtained solution was washed with water and saturated brine successively, dried over magnesium sulfate and concentrated in vacuo. The resulted residue was purified with a silica gel column chromatography (eluting solvent: n-hexane/ethyl acetate=20/1 to 3/2) to give tert-butyl cyclopropyl{[1-(3-methoxypropyl)-4-morpholin-4-yl-1H-indol-3-yl]methy}carbamate (280 mg) as a yellow oil.

1. temperatureThe reaction mixture was cooled to room temperature
2. extractionextracted with ethyl acetate
3. washThe obtained solution was washed with water and saturated brine successively
4. dry with materialdried over magnesium sulfate
5. concentrationconcentrated in vacuo
6. customThe resulted residue was purified with a silica gel column chromatography (eluting solvent: n-hexane/ethyl acetate=20/1 to 3/2)