反应详情

A solution of 3-methyl-1-[(trifluoromethyl)sulfonyl]-1H-indazol-6-yl trifluoromethanesulfonate (0.61 g, 1.5 mmol) in DMF (6 mL) was flushed with CO for 5 minutes. The solution was treated with palladium acetate (68 mg, 0.30 mmol), 1,1′-bis(diphenylphosphino)ferrocene (167 mg, 0.30 mmol), triethylamine (0.33 g, 0.45 mL, 3.2 mmol) and methanol (4 mL). The mixture was stirred at room temperature under CO (1 atm). The solution was poured into water and extracted with EtOAc (3×). The combined organic extracts were concentrated and purified by Biotage (40S column, 8% EtOAc/heptane) to provide methyl 3-methyl-1-[(trifluoromethyl)sulfonyl]-1H-indazole-6-carboxylate (330 mg, 69%).

1. extractionextracted with EtOAc (3×)
2. concentrationThe combined organic extracts were concentrated
3. custompurified by Biotage (40S column, 8% EtOAc/heptane)