反应详情

A solution of 1-(propylsulfonyl)-3-pyridin-2-ylazetidine-3-carbonitrile (II-1, 379 mg, 1.43 mmol) in 2 M NH3/MeOH (50 mL) was treated with excess Raney Ni and agitated under an atmosphere of H2 (40 psi) in a Parr apparatus. After 5 h, the reaction was filtered through Celite (MeOH wash) and concentrated under reduced pressure to afford 1-[1-(propylsulfonyl)-3-pyridin-2-ylazetidin-3-yl]methanamine (II-2) as a yellow oil. Analytical LCMS: single peak (214 nm), 1.791 min. This material was used in subsequent reactions without further purification.

1. filtrationthe reaction was filtered through Celite (MeOH wash)
2. concentrationconcentrated under reduced pressure