反应详情

A solution of methylamine (1N, 1 mL in methanol) was added to 2-(3-dimethylamino-propylamino)-8-indan-5-yl-5-oxo-5,8-dihydro-pyrido[2,3-d]pyrimidine-6-carboxylic acid ethyl ester (Example 6 Step A, 6 mg, 0.015 mmol). The mixture was kept in a sealed tube at 110° C. with stirring for 2 days. The solution, after cooling down to room temperature, was loaded to HPLC for purification (32 mL/min 5-100% MeCN/H2O gradient over 10 min). 2-(3-Dimethylamino-propylamino)-8-indan-5-yl-5-oxo-5,8-dihydro-pyrido[2,3-d]pyrimidine-6-carboxylic acid methylamide was obtained as a white solid (4.5 mg, 77%). 1H NMR (400 MHz, CDCl3) δ (ppm): 9.70 (br, 1H), 9.26 (s, 1H), 8.75 (s, 1H), 7.31 (d, J=7.8 Hz, 1H), 7.22 (s, 1H), 7.15 (d, J=7.8 Hz, 1H), 6.86 (br, 1H), 2.99 (m, 9H), 2.25-2.10 (m, 10H), 1.62 (m, 2H). Mass Spectrum (LCMS, ESI pos.) Calcd. For C23H28N6O2: 421.23 (M+H). Found. 421.1

1. customThe mixture was kept in a sealed tube at 110° C.
2. customwas loaded to HPLC for purification (32 mL/min 5-100% MeCN/H2O gradient over 10 min)