反应详情

To a solution of 4-{amino-[6-oxo-2-(3-trifluoromethyl-phenylamino)-cyclohex-1-enyl]-methyl}-3-methanesulfonyl-benzonitrile hydrochloride (INTERMEDIATE 17, 529 mg, 0.95 mmol) in acetonitrile (5.0 mL) is added 1,1′-carbonyldiimidazole (192 mg, 1.19 mmol) and triethylamine (33 μL, 0.24 mmol). After stirring at room temperature over night, the reaction mixture is concentrated under reduced pressure. The residue is treated with water and the precipitate is filtered off, washed with water and dried. Yield: 468 mg. ESI mass spectrum: [M+H]+=490; Retention time HPLC: 0.57 min (X012_S01).

1. concentrationthe reaction mixture is concentrated under reduced pressure
2. additionThe residue is treated with water
3. filtrationthe precipitate is filtered off
4. washwashed with water
5. customdried
6. custom0.57 min (X012_S01)