Water → HCID 58706654, compound

Participants

Reaction Conditions

Reaction Steps

To a solution of (S)-2-amino-2-[5-(6-bromopyridin-2-yl)thiazol-2-yl]ethanol dihydrochloride (1.00 g, 2.68 mmol) obtained in Step 3, triethylamine (3.7 ml, 2.68 mmol) in chloroform (15 ml), a solution of triphosgene (278 mg, 0.94 mmol) in chloroform (5 ml) was added dropwise while cooled to −78° C., and the mixture was stirred at the same temperature for 2 hours. The reaction solution was warmed to room temperature and water was added and it was extracted with ethyl acetate. After washed with a saturated brine, the organic layer was dried over magnesium sulfate. After concentrated, the residue was purified by flash chromatography on silica gel (chloroform:methanol:ethyl acetate=15:1:1) and the title compound (712 mg, 82%) was obtained.

Provenance & Evidence