反应详情

To a solution of (S)-methyl 3-fluoro-4-(2-oxo-1-(piperidin-4-yl)pyrrolidin-3-yloxy)benzoate hydrochloride (0.1 g, 0.29 mmol) in DMF (10 mL) was added N-ethyl-N-isopropylpropan-2-amine (0.543 mL, 2.97 mmol) and 2,3-dichloro-5-(trifluoromethyl)pyridine (0.193 g, 0.892 mmol) and the reaction was stirred overnight at ambient temperature. The reaction was diluted with EtOAc (50 mL) and washed with water (20 mL), and brine (20 mL), dried over MgSO4, filtered and concentrated under vacuum. The material was purified on silica, using a gradient of DCM to 10% EtOAc/DCM as eluent to yield (S)-methyl 4-(1-(1-(3-chloro-5-(trifluoromethyl)pyridin-2-yl)piperidin-4-yl)-2-oxopyrrolidin-3-yloxy)-3-fluorobenzoate (0.10 g, 63% yield).

1. washwashed with water (20 mL), and brine (20 mL)
2. dry with materialdried over MgSO4
3. filtrationfiltered
4. concentrationconcentrated under vacuum
5. customThe material was purified on silica