反应详情

温度

85 °C

4-bromo-3-(2-fluoro-4-methoxyphenyl)-1-methyl-1H-pyrazole-5-carbonitrile (49 mg, 0.16 mmol), tributyl(2,4-dimethylthiophen-3-yl)stannane (82.24 mg, 0.20 mmol), Pd2(dba)3 (14.44 mg, 0.02 mmol) and trio-tolylphosphine (9.6 mg, 0.03 mmol) were mixed with 1.5 mL DMF and the mixture was degassed under nitrogen in a vial. The vial was sealed and the reaction was heated at 85° C. over night. Water was added, the mixture was extracted with CH2Cl2 and the organic layer was concentrated. The crude product was purified on silica to give 4-(2,4-dimethylthiophen-3-yl)-3-(2-fluoro-4-methoxyphenyl)-1-methyl-1H-pyrazole-5-carbonitrile (17 mg, 32%).

1. customthe mixture was degassed under nitrogen in a vial
2. customThe vial was sealed
3. additionWater was added
4. extractionthe mixture was extracted with CH2Cl2
5. concentrationthe organic layer was concentrated
6. customThe crude product was purified on silica