tert-Butyl isocyanate → 3-[2-(trifluoromethyl)-4'-(methylsulfonyl)benzhydryloxy]-N-(tert-butyl)azetidine-1-carboxamide

Participants

Reaction Steps

To a solution of 3-[2-(trifluoromethyl)-4′-(methylsulfonyl)benzhydryloxy]azetidine (171) (222 mg, 0.58 mmol) in anhydrous DCM (7 mL) was added molecular sieves and tert-butyl isocyanate (68 μL, 0.58 mmol). After shaking at ambient temperature for 16 h, the mixture was poured onto a DCM-wet SCX-2 cartridge (2 g). Elution with DCM (24 mL) and evaporation afforded the desired product as a pale yellow solid (188 mg, 67%).

Provenance & Evidence