Carbonate Ion → 3-[2-(trifluoromethyl)-4'-(difluoromethoxy)benzhydryloxy]-N-(tert-butyl)azetidine-1-carboxamide

Participants

Reaction Steps

To a solution of 3-[2-(trifluoromethyl)-4′-(difluoromethoxy)benzhydryloxy]azetidine hydrochloride (175) (100 mg, 0.24 mmol) in anhydrous DCM (4 mL) was added MP-carbonate (2.62 mmol/g; 280 mg, 0.72 mmol), molecular sieves and tert-butyl isocyanate (29 μL, 0.24 mmol). After shaking at ambient temperature for 2 h, the mixture was poured onto a DCM-wet SCX-2 cartridge (2 g). Elution with DCM (20 mL) and evaporation afforded the desired product (90 mg, 78%).

Provenance & Evidence