Tetrahydrofuran → tert-Butyl 3-acetylazetidine-1-carboxylate

Participants

Reaction Conditions

Reaction Steps

To a 100 ml round bottom flask was added tert-butyl 3-{[methoxy(methyl)amino]carbonyl}azetidine-1-carboxylate (2.6 g, 10.6 mmol) and 20 ml tetrahydrofuran. The resulting solution was cooled to 0° C. and methylmagnesium chloride tetrahydrofuran solution (4.3 ml, 3M, 12.8 mmol) was added by a syringe. The reaction mixture was stirred at 0° C. for 1 hour. It was diluted with 100 ml ether, and the resulting mixture was washed twice with 100 ml saturated ammonium chloride solution. The organics were dried over sodium sulfate, filtered and concentrated. The crude product was used for the next step without further purification.

Provenance & Evidence