Ethyl Acetate → N-(4-(chlorodifluoromethoxy)phenyl)-6-(3-hydroxyazetidin-1-yl)-5-iodonicotinamide

Participants

Reaction Conditions

Reaction Steps

3-Hydroxyazetidine (164 mg, 2.18 mmol) and DIPEA (0.419 mL, 2.396 mmol) were added to a suspension of 6-chloro-N-(4-(chlorodifluoromethoxy)phenyl)-5-iodonicotinamide (Stage 48.3, 500 mg, 1.089 mmol) in iPrOH (2 mL). and stirred at 140° C. for 16 h. EtOAc (80 mL) was added and the solution was washed with 1 M HCl (30 mL), aq. sat. NaHCO3 solution (30 mL) and water (30 mL), dried over Na2SO4 and the solvent was evaporated off under reduced pressure to give the title product as yellow foam. HPLC (Condition 7) tR=6.64 min, UPLC-MS (Condition 3) tR=1.08 min, m/z=496.0/498.0 [M+H]+.

Provenance & Evidence