Ethyl (4-bromo-3,5-dimethyl-1H-pyrazol-1-yl)acetate → 2-(3,5-dimethyl-4-(6-(trifluoromethyl)-1H-indazol-4-yl)-1H-pyrazol-1-yl)acetic acid

関与物質

反応条件

反応手順

To a microwave vial were added a mixture of 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-6-(trifluoromethyl)-1H-indazole (0.3 g, 0.961 mmol), ethyl 2-(4-bromo-3,5-dimethyl-1H-pyrazol-1-yl)acetate (0.351 g, 1.346 mmol) and PdCl2(dppf) (0.035 g, 0.048 mmol) in dioxane (10 mL) and aqueous saturated NaHCO3 (3 mL). The resulting light yellow suspension was heated at 140° C. for 45 minutes in a microwave reactor. The reaction mixture was subsequently concentrated and the residue was purified by preparative HPLC, eluting with a gradient of 40-50% acetonitrile (containing 0.035% TFA) in H2O (containing 0.05% TFA) over a period of 6 minutes. Two products were separated. The product-containing fractions were combined and the volatiles removed in vacuo to give the title compound as the major product. ESI-MS m/z [M+H]+ calc'd for C15H13F3N4O2, 339.1. found 339.2.

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