Water → HCID 86668196, compound

Participants

Reaction Conditions

Reaction Steps

To a solution of 1-(3-amino-2-methoxy-5-morpholinophenyl)-2,2,2-trifluoroethanol (2.35 g, 7.67 mmol) in THF (20.4 mL), 2,2,2-trichloroethyl chloroformate (1.14 mL, 8.28 mmol), N,N-diisopropylethylamine (4.02 mL, 23.0 mmol) was added, and the mixture was stirred at 0° C. for 15 minutes. Water was added to the reaction solution and the aqueous layer was extracted with ethyl acetate. The organic layer was washed with saturated brine, dried over anhydrous sodium sulfate and filtered, and then the solvent was evaporated under reduced pressure. The obtained residue was purified by column chromatography (silica gel, hexane/ethyl acetate=80/20-60/40) to obtain 3.45 g (93% yield) of the captioned compound.

Provenance & Evidence