2-Aminopropanol → ethyl 2-(3-acetyloxy-2,4,5-trifluorobenzoyl)-3-(1-hydroxypropan-2-ylamino)prop-2-enoate

関与物質

反応手順

To 7.64 g (0.025 mole) of the ethyl 3-acetoxy-2,4,5-trifluorobenzoylacetate (VIII) thus obtained were added 20 ml of acetic anhydride and 6 ml of ortho-ethyl formate and the mixture was refluxed for 2 hours and then condensed under reduced pressure. The residue was dissolved in 50 ml of dichloromethane, added 1.91 g (0.026 mole) of DL-2-aminopropanol and allowed to stand over night. Dichloromethane was distilled under reduced pressure and the residue was applied to silica gel column chromatography (solvent: mixture of toluene:ethyl acetate=1:1) to give 4.37 g of the ethyl-2-(3-acetoxy-2,4,5-trifluorobenzoyl)-3-(2-hydroxy-1-methylethyl)aminoacrylate (X) as pale yellow oily product. ##STR10##

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