反应详情

温度

120 °C

A mixture of 3-iodo-1-(tetrahydro-2H-pyran-2-yl)-1H-indazole-4-carbonitrile (50 mg, 0.142 mmol), K3PO4 (61.34 mg, 0.284 mmol), Pd(dppf)Cl2 (10.3 mg, 0.0142 mmol), 2,4,6-trimethyl-1,3,5,2,4,6-trioxatriborinane (18 mg, 0.142 mmol) in DMF (0.5 mL) under nitrogen in a sealed vial was heated at 120° C. in a microwave oven for 100 minutes. The reaction mixture was filtered and the filtrate diluted with H2O and extracted with EtOAc. The combined extracts extracts were dried (MgSO4), filtered, and concentrated in vacuo to afford 3-methyl-1-(tetrahydro-2H-pyran-2-yl)-1H-indazole-4-carbonitrile as white solid (12 mg, 35.5%). MS (ESI): m/z=242 [M+1]+.

1. filtrationThe reaction mixture was filtered
2. additionthe filtrate diluted with H2O
3. extractionextracted with EtOAc
4. dry with materialThe combined extracts extracts were dried (MgSO4)
5. filtrationfiltered
6. concentrationconcentrated in vacuo