反应详情

温度

150 °C

3-(3-Bromo-imidazo[1,2-a]pyridin-6-ylmethyl)-6-(1-methyl-1H-pyrazol-4-yl)-imidazo[1,2-b]pyridazine (Example 296, 50 mg, 0.122 mmol) was dissolved in dioxane (0.5 mL) in a microwave reactor. Then tributyl(vinyl)tin (36.9 μL, 0.122 mmol) and tetrakis(triphenylphosphine)palladium (1.4 mg, 0.001 mmol) were introduced. The RM was heated at 150° C. for 30 min under microwave irradiations. The solvent was removed and The residue was purified by preparative HPLC with acetonitrile and water (+0.1% TFA). The fractions were joined and were lyophilized. The residue was dissolved in MeOH and it was passed through an SPE cartridge of HCO3− to remove the TFA salt. The filtrate was evaporated to give the free salt of the title compound as a yellow solid (tR 0.7 min (conditions 2), MH+=356).

1. customThe solvent was removed
2. customThe residue was purified by preparative HPLC with acetonitrile and water (+0.1% TFA)
3. dissolutionThe residue was dissolved in MeOH
4. customto remove the TFA salt
5. customThe filtrate was evaporated