反应详情

A solution of 3.88 g of ethyl 4-[2-(dimethylaminomethyl)-morpholino]-2,3,5-trifluorobenzoylacetate and 1.85 g of dimethylformamide dimethylacetal in 20 ml of toluene is refluxed for 6 hours. The reaction mixture is concentrated under reduced pressure and to the obtained residue is added 20 ml of ethanol. After the addition of 0.94 g of cyclopropylamine under ice-cooling, the mixture is stirred at room temperature for 3 hours. The reaction mixture is concentrated under reduced pressure and the obtained residue is purified by chromatography on silica gel to give 4.06 g of ethyl 2-[4-[2-(dimethylaminomethyl)morpholino]-2,3,5-trifluorobenzoyl]-3-cyclopropylaminoacrylate in 89% yield as an oily substance.

1. concentrationThe reaction mixture is concentrated under reduced pressure and to the obtained residue
2. additionis added 20 ml of ethanol
3. additionAfter the addition of 0.94 g of cyclopropylamine under ice-
4. temperaturecooling
5. concentrationThe reaction mixture is concentrated under reduced pressure
6. customthe obtained residue is purified by chromatography on silica gel