反应详情

温度

100 °C

To a solution of 3-(2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl)-pentanoic acid methyl ester (50 mg, 0.18 mmol) (prepared according to example 2, steps 1-2) in DMF (10 mL) are added 3-bromomethyl-4,6-dimethyl-1,2-benzisothiazole (70 mg, 0.271 mmol) and K2CO3 (50 mg, 0.36 mmol) at room temperature under a nitrogen atmosphere. The solution is heated at 100° C. for 2 hours. The solution is cooled down and water is added. The solution is extracted with EtOAc and the combined organic layer is dried with MgSO4. The solution is filtered and the filtrate is concentrated. The residue is purified by flash chromatography with 20% EtOAc in Hexane as the eluent to afford 3-[1-(4,6-Dimethyl-1,2-benzisothiazol-3-ylmethyl)-2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl]-pentanoic acid methyl ester (65 mg, 80%) as a colorless foam.

1. temperatureThe solution is cooled down
2. extractionThe solution is extracted with EtOAc
3. dry with materialthe combined organic layer is dried with MgSO4
4. filtrationThe solution is filtered
5. concentrationthe filtrate is concentrated
6. customThe residue is purified by flash chromatography with 20% EtOAc in Hexane as the eluent