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

Participants

Reaction Conditions

Reaction Steps

A mixture of tert-butyl 3-iodoazetidine-1-carboxylate (EP 1176147, prep 18) (5 g, 17.6 mmol) and dimethylamine (27 mL, 33% in ethanol, 176 mmol) was heated to 80° C. for 28 hours in a sealed vessel. The cooled mixture was evaporated in vacuo and the residue pre-adsorbed onto silica gel. This was then purified by column chromatography on silica gel using ethyl acetate:hexane (50:50) as eluant to afford the title compound as a yellow oil, 1.07 g.

Provenance & Evidence