Acetic Anhydride → HCID 89730082, compound

Participants

Reaction Conditions

Reaction Steps

To a solution of tert-butyl azetidin-3-ylcarbamate (100 g, 0.58 mol) and Et3N (88 g, 0.87 mol) in DCM (1500 mL) was added Ac2O (59.6 g, 0.88 mol) dropwise at 0° C. The mixture was then stirred at 0° C. for 2 h, at which time TLC showed the completion of the reaction. The reaction was quenched by addition of water (1000 mL) and then stirred at 20° C. for 30 min. The organic phase was separated, dried (Na2SO4) and concentrated to give the crude product. Seven batches were run in parallel and produced a combined crude product weight of 530 g. This crude was used in next step without the further purification. LCMS (m/z): 215.1 (M+1).

Provenance & Evidence