反应详情

A mixture of 5-chloro-3-cyclohexyl-8-iodo-1,2-dihydro-1,2,4-benzothiadiazine-1,1-dioxide (290 mg, 0.68 mmol), 2-methoxyphenylboronic acid (122 mg, 0.80 mmol), Pd(PPh3)2Cl2 (10 mg, 2 mol %) in 1,2-dimethoxyethane (50 ml) and Na2CO3 (2M, 2 ml, 4 mmol) were refluxed under N2 for 2 h. The solvents were removed under reduced pressure and the residue was extracted with EtOAc (2×40 ml) and the organic layer was washed with saturated NaHCO3 (20 ml), dried (Na2SO4) and the solvent was removed under reduced pressure. The product was purified by flash chromatography on SiO2 using EtOAc:n-hexane (1:2, v/v) as eluent, yielding 200 mg (73%) of 5-chloro-3-cyclohexyl-8-(2-methoxyphenyl)-1,2-dihydro-1,2,4-benzothiadiazine-1,1-dioxide as colorless crystals.

1. temperaturewere refluxed under N2 for 2 h
2. customThe solvents were removed under reduced pressure
3. extractionthe residue was extracted with EtOAc (2×40 ml)
4. washthe organic layer was washed with saturated NaHCO3 (20 ml)
5. dry with materialdried (Na2SO4)
6. customthe solvent was removed under reduced pressure
7. customThe product was purified by flash chromatography on SiO2