Nitrogen → (3-[2-[2-Amino-6-(4-methylpiperazin-1-yl)pyrimidin-4-yl]-3-methyl-1,2,3,4-tetrahydroisoquinolin-7-yl)-1H-pyrazol-1-yl)acetonitrile

Beteiligte Stoffe

Reaktionsbedingungen

Reaktionsschritte

A mixture of (3-bromo-1H-pyrazol-1-yl)acetonitrile (14.4 mg, 0.0775 mmol), 4-(4-methylpiperazin-1-yl)-6-[3-methyl-7-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-3,4-dihydroisoquinolin-2(1H)-yl]pyrimidin-2-amine (18.0 mg, 0.0388 mmol), dichloro(bis{di-tert-butyl[4-(dimethylamino)phenyl]phosphoranyl})palladium (1.0 mg, 0.0014 mmol), and sodium carbonate (8.22 mg, 0.0775 mmol) in 1,4-dioxane (0.5 mL) and water (0.1 mL) was vacuumed and refilled with N2 for 3 times and then stirred at 90° C. overnight. The mixture was purified by RP-HPLC (pH=10) to afford the desired product. LCMS (M+H)+: m/z=444.2.

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