Cyclopropylamine → ethyl 3-(cyclopropylamino)-2-(2,3,4,5-tetrafluoro-6-methylbenzoyl)prop-2-enoate

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Reaction Steps

Ethyl 2-(6-methyl-2,3,4,5-tetrafluorobenzoyl)-3-ethoxyacrylate (5 g) is dissolved in ethanol (25 ml) and thereto cyclopropylamine (1.0 g) is added dropwise under ice-cooling. After stirring at room temperature for 30 minutes, the mixture is concentrated and the residue is purified with column chromatography (silica-gel, dichloromethane : n-hexane=1 : 1) to give ethyl 2-(6-methyl-2,3,4,5-tetrafluorobenzoyl)-3 -cyclopropylaminoacrylate (4.74 g), as white plates, m.p. 78°-79° C. (recrystallized from petroleum ether--n-hexane).

Provenance & Evidence