Triethylamine → Tert-butyl 3-(dimethylamino)azetidine-1-carboxylate

Participants

Reaction Steps

To a solution of N,N-dimethylazetidin-3-amine (Intermediate 28, 100 g, 1.0 mol) and triethylamine (487 mL, 3.5 mol) in CH2Cl2 (500 mL) was added tert-butyl (2-methylpropan-2-yl)oxycarbonyl carbonate (326 g, 1.5 mol) at 0° C. The mixture was then stirred at r.t. for 5 h. The mixture was then washed with water (4×500 mL) and the organic solution were dried (Na2SO4) and concentrated in vacuo. Purification by FCC gave the title compound (62 g, 31%).

Provenance & Evidence