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 (53 mg, 0.174 mmol) and 5-chloro-1,3-dihydro-indol-2-one (29 g, 0.84 mmol) was dissolved in 0.9 ml of ethanol under stirring, and added with piperidine (0.1 ml, 1.0 mmol) to the solution at room temperature. The mixture was heated to reflux for 2 hours in an oil bath and lots of precipitates were formed. Then the ice-salt bath was removed, and the reaction mixture was naturally cooled down to room temperature, filtered to obtain the title compound (Z)-2-(5-chloro-2-oxo-1,2-dihydro-indol-3-ylidenemethyl)-3-methyl-5-(2-morpholin-4-yl-ethyl)-5,6,7,8-tetrahydro-1H-pyrrolo[3,2-c]azepin-4-one 10 (30 g, yield 38%) as a red solid.

1. temperatureThe mixture was heated
2. temperatureto reflux for 2 hours in an oil bath
3. customlots of precipitates
4. customwere formed
5. customThen the ice-salt bath was removed
6. filtrationfiltered