反应详情

温度

180 °C

300 mg (0.71 mmol) of methyl 4-{[(3-bromo-2,6-dichlorophenyl)acetyl]amino}-1,3-thiazole-5-carboxylate and 230 mg (1.41 mmol) of (5-chloro-2-thienyl)boronic acid were dissolved in a mixture of 18 ml of toluene and 3 ml of water, and 450 mg (2.12 mmol) of potassium phosphate, 15.9 mg (0.07 mmol) of palladium acetate and 20 mg (0.07 mmol) of tricyclohexylphosphine were added in succession. With microwave irradiation, the reaction mixture was then heated at 180° C. for 1 h. The mixture was filtered and the filtrate was taken up in ethyl acetate and water. The organic phase was dried and concentrated by evaporation. This gave 170 mg of methyl 4-({[2,6-dichloro-3-(5-chloro-2-thienyl)phenyl]acetyl}amino)-1,3-thiazole-5-carboxylate, which were reacted further without further purification.

1. additionwere added in succession
2. customWith microwave irradiation
3. filtrationThe mixture was filtered
4. customThe organic phase was dried
5. concentrationconcentrated by evaporation
6. customThis gave 170 mg of methyl 4-({[2,6-dichloro-3-(5-chloro-2-thienyl)phenyl]acetyl}amino)-1,3-thiazole-5-carboxylate, which were reacted further without further purification