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With tetrakis(triphenylphosphine) palladium(0); potassium carbonate; In 1,4-dioxane; water; at 95.0℃; for 2.0h;Sealed tube;
Example 2881 -(3-[2-amino-6-(4-methyl-1 H-indazol-5-yl)pyrimidin-4-yl]amino}propyl)pyrrolidin-2-one.A mixture of 1 -{3-[(2-amino-6-chloropyrimidin-4-yl)amino]propyl}pyrrolidin-2-one (27 mg, 0.10 mmol), (4-methyl-i H-indazol-5-yl)boronic acid (19 mg, 0.11 mmol), potassium carbonate (28 mg, 0.20 mmol) and palladium tetrakis(triphenylphosphine)palladium (0) (6 mg, 0.005 mmol) in 1,4-dioxane (4 mL) and water (1 mL) was heated in a sealed tube at 95C for 2 h. The reactionmixture was concentrated and purified by preparative HPLC. LCMS [M+H] 366.
With tetrakis(triphenylphosphine) palladium(0); potassium carbonate; In 1,4-dioxane; water; at 95.0℃; for 2.0h;Sealed tube;
Example 288 1- (3-[2-amino-6-(4-methyl-1 H-indazol-5-yl)pyrimidin-4-yl]amino}propyl)pyrrolidi 2- one. A mixture of 1-{3-[(2-amino-6-chloropyrimidin-4-yl)amino]propyl}pyrrolidin-2-one (27 mg, 0.10 mmol), (4-methyl-1 H-indazol-5-yl)boronic acid (19 mg, 0.1 1 mmol), potassium carbonate (28 mg, 0.20 mmol) and palladium tetrakis(triphenylphosphine)palladium (0) (6 mg, 0.005 mmol) in 1 ,4-dioxane (4 ml_) and water (1 ml_) was heated in a sealed tube at 95C for 2 h. The reaction mixture was concentrated and purified by preparative HPLC. LCMS [M+H]+ 366.
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