反应详情

温度

140 °C

4-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-6-(trifluoromethyl)-1H-indazole (58.3 mg, 0.187 mmol), 2-(4-bromo-3,5-dimethyl-1H-pyrazol-1-yl)-N-isopropylacetamide (77 mg, 0.28 mmol), PdCl2(dppf) (13.66 mg, 0.019 mmol), sodium bicarbonate (0.399 mL, 0.747 mmol), and dioxane (2 mL) were mixed in a 10 mL vial to give an orange suspension. The vial was sealed and then heated to 140° C. for 45 minutes in a microwave reactor. The reaction mixture was subsequently filtered and the product was purified by preparative HPLC, eluting with a gradient of 35-55% ACN (containing 0.035% TFA) in H2O (containing 0.05% TFA). The pure fractions were lyophilized to give a TFA salt of the title compound as a white solid (10.2 mg, 11.1%). 1H NMR (400 MHz, CD3OD) δ ppm 1.20 (d, J=6.57 Hz, 6H), 2.15 (s, 3H), 2.19 (s, 3H), 2.66 (s, 1H), 7.23 (s, 1H), 7.87 (s, 1H), 8.00 (d, J=1.01 Hz, 1H); ESI-MS m/z [M+H]+ calc'd for C18H20F3N5O, 380.2. found 380.3.

1. customto give an orange suspension
2. customThe vial was sealed
3. filtrationThe reaction mixture was subsequently filtered
4. customthe product was purified by preparative HPLC
5. washeluting with a gradient of 35-55% ACN (containing 0.035% TFA) in H2O (containing 0.05% TFA)