2-(1-((4-Morpholino-2-(tributylstannyl)pyrido[3,2-d]pyrimidin-6-yl)methyl)piperidin-4-yl)propan-2-ol → 2-(1-((2-(2-ethyl-2H-indazol-3-yl)-4-morpholinopyrido[3,2-d]pyrimidin-6-yl)methyl)piperidin-4-yl)propan-2-ol

Participants

Reaction Steps

To a degassed solution of 2-(1-((4-morpholino-2-(tributylstannyl)pyrido[3,2-d]pyrimidin-6-yl)methyl)piperidin-4-yl)propan-2-ol (0.13 g) and 2-ethyl-3-iodo-2H-indazole (1.05 eq) in 1,4-dioxane (1.5 mL) was added copper(I) thiophene-2-carboxylate (1 eq) and tetrakis(triphenylphosphine)palladium(0) (0.05 eq). The reaction was microwaved at 140° C. for 30 minutes and then loaded onto Biotage isolute scx-2 catridge and eluted with 2M ammonia in Methanol. The crude material was purified by reverse phase HPLC to afford 36.6 mg of 136. MS (Q1) 516.3 (M)+

Provenance & Evidence