反应详情

A mixture of compound 2-(2-acetylhydrazinecarbonyl)-5-bromo-N-methyl-6-(N-methylmethylsulfonamido)benzofuran-3-carboxamide (150 mg, 0.33 mmol), p-TsCl (124 mg, 0.66 mmol) and Et3N (108 mg, 0.98 mmol) in CH2Cl2 (6 mL) was refluxed for 5 h. After concentration in vacuo, the residue was purified with prep-TLC (DCM:MeOH=100:1) to give the product 5-bromo-N-methyl-2-(5-methyl-1,3,4-oxadiazol-2-yl)-6-(N-methylmethylsulfonamido)benzofuran-3-carboxamide (146 mg, yield: 63%). 1H-NMR (CDCl3, 400 MHz) δ 9.80 (br s, 1H), 8.96 (s, 1H), 7.77 (s, 1H), 3.36 (s, 3H), 3.13˜3.06 (m, 6H), 2.75 (s, 3H). MS (M+H)+: 443/445.

1. temperaturewas refluxed for 5 h
2. concentrationAfter concentration in vacuo
3. customthe residue was purified with prep-TLC (DCM:MeOH=100:1)