Triphenylphosphine → tert-butyl {(1S)-2-[(6-chloro-5-fluoropyridin-3-yl)oxy]-1-methylethyl}carbamate

Participants

Reaction Steps

To a mixture of 6-chloro-5-fluoropyridin-3-ol (2.43 g), tert-butyl [(1S)-2-hydroxy-1-methylethyl]carbamate (3.46 g), triphenylphosphine (6.48 g) and THF (25 mL) was added dropwise a toluene solution (1.9 M, 13.0 mL) of diisopropyl azodicarboxylate at room temperature, and the obtained mixture was stirred at room temperature for 3 days. The reaction mixture was concentrated under reduced pressure, and the residue was purified by silica gel column chromatography (hexane/ethyl acetate) to give the title compound (2.88 g).

Provenance & Evidence