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 (80 mg, 0.26 mmol) and 5-(4-fluoro-phenylmethanesulfonyl)-1,3-dihydro-indol-2-one 65a (72 mg, 0.24 mmol) were dissolved in 2.5 ml of ethanol, and added with 42 μA of piperidine the solution at room temperature. Upon completion of the addition, the reaction mixture was heated to reflux for 3 hours. After thin lay chromatography showed the disappearance of starting materials, the reaction mixture was naturally cooled 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-(4-fluorobenzylsulfonyl)-2-oxoindolin-3-ylidene)methyl)-3-methyl-5-(2-morpholinoethyl)-5,6,7,8-tetrahydropyrrolo[3,2-c]azepin-4(1H)-one 69 (120 mg, yield 85.7%) as an orange solid.

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