反应详情

A mixture of 1-cyclohexyl-5-(piperidin-1-ylmethyl)-1H-benzo[d]imidazol-2-amine (420 mg, 0.00134 mol), 5-bromo-3-iodo-1-((2-(trimethylsilyl)ethoxy)methyl)-1H-indazole (916 mg, 0.00202 mol), xantphos (237 mg, 0.000410 mol), tris(dibenzylideneacetone)dipalladium(0) (147 mg, 0.000160 mol), and potassium phosphate (510 mg, 0.00240 mol) in 1,4-Dioxane (6.0 mL) was flushed with argon. The mixture was microwaved at 300 watts, 130° C. for 15 minutes. The reaction mixture was filtered, concentrated and purified by preparative HPLC to yield 582 mg of 5-bromo-N-(1-cyclohexyl-5-(piperidin-1-ylmethyl)-1H-benzo[d]imidazol-2-yl)-1-((2-(trimethylsilyl)ethoxy)methyl)-1H-indazol-3-amine as the bis-TFA salt.

1. customwas flushed with argon
2. customThe mixture was microwaved at 300 watts, 130° C. for 15 minutes
3. filtrationThe reaction mixture was filtered
4. concentrationconcentrated
5. custompurified by preparative HPLC