反应详情

Phosphorus oxychloride (0.21 g, 1.38 mmol) is added drop wise at 0° C. to a solution of (S)-1-(4-chloro-phenyl)-azepane-2-carboxylic acid (0.23 g, 0.92 mmol) and 5-tert-butyl-isoxazol-3-ylamine (0.19 g, 1.38 mol) in pyridine. The reaction mixture is slowly warmed up to room temperature and stirred for three hours. The mixture is diluted with EtOAc and washed twice with saturated NH4Cl solution. The organic phase is washed with 1N HCl, and after drying over anhydrous Na2SO4 the solvent is removed under reduced pressure to afford the crude product that is purified by prep TLC to afford the title compound; m/z 376 [M+H+].

1. washwashed twice with saturated NH4Cl solution
2. washThe organic phase is washed with 1N HCl
3. dry with materialafter drying over anhydrous Na2SO4 the solvent
4. customis removed under reduced pressure
5. customto afford the crude product that
6. customis purified by prep TLC