Ethyl 3-chloro-3-oxopropionate → ethyl 3-((2-acetyl-5-(trifluoromethyl)phenyl)(tetrahydro-2H-pyran-4-yl)amino)-3-oxopropanoate

Participants

Reaction Conditions

Reaction Steps

To a stirred solution of 400 mg (1.39 mmol) 1-(2-(tetrahydro-2H-pyran-4-ylamino)-4-(trifluoromethyl)phenyl)ethanone in benzene (5 ml) was added 360 μl (2.78 mmol) ethyl 3-chloro-3-oxopropanoate at 0° C. The reaction mixture was stirred at 80° C. for 4 h. Then the mixture was diluted with ethyl acetate (20 ml) and washed with water (20 ml), brine (20 ml), a sat. aq. Na2CO3 sol. (2×30 ml), dried over anhydrous Na2SO4 and concentrated in vacuo to yield 550 mg (1.37 mmol, 98%) ethyl 3-((2-acetyl-5-(trifluoromethyl)phenyl)(tetrahydro-2H-pyran-4-yl)amino)-3-oxopropanoate, which was used in the next step without further purification.

Provenance & Evidence