反应详情

温度

100 °C

To a solution of (R)-3-(2-oxo-2,3-dihydro-imidazo[4,5-c]pyridin-1-yl)-3-phenyl-propionic acid ethyl ester (refer to example 2) (50 mg, 0.16 mmol) in DMF (10 mL) were added 3-Bromomethyl-4,6-dimethyl-benzo[d]isothiazol (62 mg, 0.24 mmol) and K2CO3 (44 mg, 0.32 mmol) at room temperature under nitrogen atmosphere. The solution was heated to 100° C. for 2 hours. The solution was cooled and water was added. The solution was extracted with EtOAc and the combined organic layer was dried with MgSO4. The solution was filtered and concentrated. The residue was purified by silica gel flash column chromatography with 20% EtOAc in Hexane as the eluent to afford the title compound (15 mg, 90%) as colorless foam.

1. temperatureThe solution was cooled
2. extractionThe solution was extracted with EtOAc
3. dry with materialthe combined organic layer was dried with MgSO4
4. filtrationThe solution was filtered
5. concentrationconcentrated
6. customThe residue was purified by silica gel flash column chromatography with 20% EtOAc in Hexane as the eluent