反应详情

温度

100 °C

To a 25 ml two-necked flask equipped with a reflux condenser and in Argon atmosphere, were added 1-(2-chloroethyl)-3,4-dihydro-7-fluoro-3-(1-methylethyl)-1H-2,1,3-benzothiadiazine-2,2-dioxide(678 mg, 2.2 mmol), 4-(6-fluoroindol-3-yl)-1,2,5,6-tetrahydropyridine (523 mg, 242 mmol), anhydrous K2CO3 (1.09 g, 11 mmol) and 10 ml of deionised water. The mixture was vigorously stirred under Argon for 64 hours at 100° C., allowed to reach room temperature and extracted with EtOAc (3×25 ml). The combined organic extracts were dried (Na2SO4) and solvent removed at reduced pressure. The residue was purified by flash chromatography on silica gel (EtOAc:hexane 1:3) affording 3,4-dihydro-1-{2-[4-(6-fluoroindol-3-yl)-1,2,5,6-tetrahydro-1-pyridyl]-1-ethyl}-3-(1-methylethyl)-7-fluoro-1H-2,1,3-benzothiadiazine-2,2-dioxide as a pale yellow solid, m.p. 103-105°.

1. customTo a 25 ml two-necked flask equipped with a reflux condenser and in Argon atmosphere
2. customto reach room temperature
3. extractionextracted with EtOAc (3×25 ml)
4. dry with materialThe combined organic extracts were dried (Na2SO4) and solvent
5. customremoved at reduced pressure
6. customThe residue was purified by flash chromatography on silica gel (EtOAc:hexane 1:3)