Azetidine → Methyl 3-(azetidin-1-ylsulfonyl)-5-(trifluoromethyl)benzoate

Participants

Reaction Steps

To a solution of methyl 3-(chlorosulfonyl)-5-(trifluoromethyl)benzoate (0.3 g, 991 μmol; Buttpark Ltd.) in CH2Cl2 (1 mL) were added DIPEA (192 mg, 260 μL, 1.49 mmol) and azetidine (62.3 mg, 73.5 μL, 1.09 mmol). The clear, light yellow solution was stirred at room temperature for 4 hours and then poured on saturated aqueous NH4Cl solution and EtOAc and the layers were separated. The aqueous layer was extracted twice with EtOAc. The organic layers were dried over MgSO4, filtered, and evaporated. Light brown solid (0.316 g; 98%). MS (EI): m/z=323 [M].

Provenance & Evidence