تفاعل #682853

معادلة التفاعل

5-bromo-2-iodo-N-methyl-6-(N-methylmethylsulfonamido)benzofuran-3-carboxamide

2-methylthiazole

Na2CO3

→

5-bromo-N-methyl-6-(N-methylmethylsulfonamido)-2-(2-methylthiazol-5-yl)benzofuran-3-carboxamide

المردود 43.6%

المذيبات

DMF

ظروف التفاعل

المعالجة

1. 1
   أخرىAfter the solvent was removed
2. 2
   أخرىthe residue was purified by column chromatography (DCM:EtOAc=2:1)

الإجراء التجريبي

To a degassed solution of compound 5-bromo-2-iodo-N-methyl-6-(N-methylmethylsulfonamido)benzofuran-3-carboxamide (600 mg, 1.2 mmol), 2-methylthiazole (244 mg, 2.5 mmol) and Na2CO3 (261 mg, 2.5 mmol) in DMF (6 mL) was added Pd(dppf)Cl2 (50 mg) under N2, and the mixture was stirred at 80° C. for 12 h. After the solvent was removed, the residue was purified by column chromatography (DCM:EtOAc=2:1) to give the product of 5-bromo-N-methyl-6-(N-methylmethylsulfonamido)-2-(2-methylthiazol-5-yl)benzofuran-3-carboxamide (240 mg, yield: 42%). 1H-NMR (CDCl3, 400 MHz) δ 8.36 (s, 1H), 7.98˜8.01 (m, 1H), 7.68 (s, 1H), 6.06 (br s., 1H), 3.33 (s, 3H), 3.10 (s, 3H), 3.08 (d, J=5.2 Hz, 3H), 2.78 (s, 3H). MS (M+H)+: 458/460.

المصدر