2,4-Dichloropyrimidine → 2-Chloro-4-(3-(4-fluorophenoxy)azetidin-1-yl)pyrimidine

Participants

Reaction Conditions

Reaction Steps

To 2,4-dichloropyrimidine (200.0 mg, 1.342 mmol) in 2-propanol (7 mL) at 0° C. was added N-ethyl-N-isopropylpropan-2-amine (0.702 mL, 4.03 mmol) followed by 3-(4-fluorophenoxy)azetidine hydrochloride (273 mg, 1.342 mmol). The resulting reaction mixture was stirred at 0° C. for 10 min then at RT for 41 h and concentrated. Purification of the crude product was done using MPLC (25 g cartridge, 40 g column, 0 to 60% EtOAc-hexanes) to give 2-chloro-4-(3-(4-fluorophenoxy)azetidin-1-yl)pyrimidine (314.2 mg).

Provenance & Evidence