反应详情

温度

80 °C

To a solution of 6-bromo-2-(4-cyclopropylpiperazin-1-yl)benzothiazole (500 mg, 1.48 mmol) and 5-chloro-2-methoxypyridin-4-yl-4-boronic acid (334 mg, 1.78 mmol) in DMF (20 mL) was added PdCl2(dppf) (108 mg, 0.148 mmol), followed by CH3COOK (581 mg, 5.92 mmol). The mixture was heated at 80° C. for 2 h, filtered and the volatiles evaporated. Water (5 mL) was added and the mixture was extracted with CH2Cl2 (3×5 mL). The combined organic extracts were dried (Na2SO4) and concentrated. The residue was purified by the preparative HPLC to give 35 mg (6%) of 6-(5-chloro-2-methoxypyridin-4-yl)-2-(4-cyclopropylpiperazin-1-yl)benzothiazole as a trifluoroacetate salt.

1. filtrationfiltered
2. customthe volatiles evaporated
3. additionWater (5 mL) was added
4. extractionthe mixture was extracted with CH2Cl2 (3×5 mL)
5. dry with materialThe combined organic extracts were dried (Na2SO4)
6. concentrationconcentrated
7. customThe residue was purified by the preparative HPLC