6-Amino-3-oxo-2,3-dihydro-indazole-1-carboxylic acid tert-butyl ester → 6-[4-(5-Cyclopropyl-2H-pyrazol-3-ylamino)-5-phenyl-pyrimidin-2-ylamino]-1,2-dihydro-indazol-3-one

Participants

Reaction Conditions

Reaction Steps

To ((2-Chloro-5-phenyl-pyrimidin-4-yl)-(5-cyclopropyl-2H-pyrazol-3-yl)-amine (75 mg, 0.241 mmol), was added 6-Amino-3-oxo-2,3-dihydro-indazole-1-carboxylic acid tert-butyl ester (180 mg, 0.72 mmol) in n-butanol and the solution was heated to 95° C. in a sealed tube. After 12 hr, the solution was concentrated and the title compound was isolated by preparative HPLC as a white solid (5.2 mg, 5% yield) HNMR (500 MHz, MeOH d-6). 7.82-7.80 (2H, m), 7.59-7.50 (6H, m), 7.19-7.17 (1H, m), 6.08 (1H, s), 2.65 (1H, m), 0.91-0.89 (2H, m), 0.45 (2H, m); LCMS m/e: 1.9 min, 425.1 (M+H), 423.1 (M-H).

Provenance & Evidence