反应详情

To a solution of 62.8 mg (0.4 mmol) of 4-tert-butyl-thiazol-2-ylamine in DCM (2 mL) were added 98 mg (0.6 mmol) of 1,1′-carbonyldiimidazole and the reaction was stirred for 4 h at room temperature. A solution of 354 mg (0.8 mmol) of [1,4]diazepan-1-yl-(tetrahydro-pyran-4-yl)-methanone (triple trifluoroacetic acid salt, prepared according to Method L, above) in DCM (3 mL) was added and the reaction stirred for 18 h at room temperature. The reaction mixture was washed with 10% aqueous citric acid solution (5 mL). The organic layer was dried over Na2SO4, filtered and the filtrate was concentrated under reduced pressure. The crude product was purified by mass-triggered preparative LCMS to afford 27.6 mg of 4-(tetrahydro-pyran-4-carbonyl)-[1,4]diazepane-1-carboxylic acid (4-tert-butyl-thiazol-2-yl)-amide.

1. stirringthe reaction stirred for 18 h at room temperature
2. washThe reaction mixture was washed with 10% aqueous citric acid solution (5 mL)
3. dry with materialThe organic layer was dried over Na2SO4
4. filtrationfiltered
5. concentrationthe filtrate was concentrated under reduced pressure
6. customThe crude product was purified by mass-triggered preparative LCMS