反应详情

3-Methyl-5-(2-morpholin-4-yl-ethyl)-4-oxo-1,4,5,6,7,8-hexahydro-pyrrolo[3,2-c]azepine-2-carbaldehyde 10c (100 mg, 0.325 mmol) and 5-(2,6-dichloro-phenylmethanesulfonyl)-1,3-dihydro-indol-2-one 64c (104 mg, 0.293 mmol) were dissolved in 3 ml of ethanol, and added with 52 μl of piperidine to the solution at room temperature. Upon completion of the addition, the reaction mixture was heated to reflux for 2 hours. After thin lay chromatography showed the disappearance of starting materials, the reaction mixture was naturally cooled down to room temperature and filtered. The filter cake was washed with anhydrous ethanol (3 ml×2) and dried to obtain the title compound (Z)-2-(5-(2,6-dichlorobenzylsulfonyl)-2-oxoindolin-3-yl idene)methyl)-3-methyl-5-(2-morpholinoethyl)-5,6,7,8-tetrahydropyrrolo[3,2-c]azepin-4(1H)-one 64 (166 mg, yield 88%) as an orange solid.

1. additionUpon completion of the addition
2. temperaturethe reaction mixture was heated
3. temperatureto reflux for 2 hours
4. filtrationfiltered
5. washThe filter cake was washed with anhydrous ethanol (3 ml×2)
6. customdried