Methylamine → 2-[4-(3-Dimethylamino-2-hydroxy-propoxy)-phenylamino]-8-indan-5-yl-5-oxo-5,8-dihydro-pyrido[2,3-d]pyrimidine-6-carboxylic acid methylamide

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Reaction Conditions

Reaction Steps

To a solution of 2-[4-(3-dimethylamino-2-hydroxy-propoxy)-phenylamino]-8-indan-5-yl-5-oxo-5,8-dihydro-pyrido[2,3-d]pyrimidine-6-carboxylic acid ethyl ester (from Example 2(c), 8 mg) in 1 mL of methanol was added 1 mL of methylamine (40 wt. % in water). The solution was stirred at 70° C. for 30 minutes. The solvent was evaporated to yield a yellow solid (6.6 mg). 1H NMR (400 MHz, CDCl3) δ (ppm): 9.64 (m, 1H), 9.35 (s, 1H), 8.82 (s, 1H), 7.39 (m, 2H), 7.27 (m, 1H), 7.15 (m, 2H), 6.66 (br, 2H), 4.06 (m, 1H), 3.93 (m, 2H), 3.02 (m, 5H), 2.89 (m, 4H), 2.56 (dd, 1H), 2.35 (m, 7H), 2.22 (m, 2H). Mass Spectrum (LCMS, ESI pos.) Calcd. For C29H32N6O4: 529.25 (M+H), Found: 529.2.

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