Water → HCID 86668195, compound

Participants

Reaction Conditions

Reaction Steps

A solution of crude product (0.397 g) containing 1-(3-amino-5-tert-butyl-2-methoxyphenyl)-2,2,2-trifluoroethanol and N,N-diisopropylethylamine (0.374 mL, 2.14 mmol) in THF (4.77 mL) was cooled to 0° C., and 2,2,2-trichloroethyl chloroformate (0.217 mL, 1.57 mmol) was added thereto, followed by stirring the mixture for 10 minutes. Water was added to the reaction solution and the aqueous layer was extracted with ethyl acetate and the organic layer was washed with saturated brine. The organic layer was 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=100/0-75/25) to obtain 0.622 g of the captioned compound (96% yield in 2 steps).

Provenance & Evidence