反应详情

温度

120 °C

Prepared similarly to that described in Example 210 using 2-(3-fluoroquinoxalin-5-yl)-6,7-dihydro-1H-pyrrolo[3,2-c]pyridin-4(5H)-one (Example 210i; 110 mg, 0.390 mmol), 2,2-dimethylpiperidine hydrochloride (117 mg, 0.779 mmol, Anichem, North Brunswick, N.J.), and DIPEA (339 μl, 1.948 mmol), heating at 120° C. for 5 h. Purification by rpHPLC (Phenomenex Gemini C18, 10 μm, 150×30 mm; 10-100% ACN/water with 0.1% TFA) provided 2-(3-(2,2-dimethylpiperidin-1-yl)quinoxalin-5-yl)-6,7-dihydro-1H-pyrrolo[3,2-c]pyridin-4(5H)-one (14% yield). 1H NMR (400 MHz, DMSO-d6) δ ppm 1.48 (s, 6H) 1.61-1.82 (m, 6H) 2.87 (t, J=6.85 Hz, 2H) 3.45 (td, J=6.80, 2.45 Hz, 2H) 3.61-3.66 (m, 2H) 6.96 (br. s., 1H) 7.09 (d, J=2.35 Hz, 1H) 7.52 (t, J=7.82 Hz, 1H) 7.73 (dd, J=8.12, 1.27 Hz, 1H) 7.93 (dd, J=7.43, 1.37 Hz, 1H) 8.78 (s, 1H) 11.76 (br. s., 1H). MS (ESI, pos. ion) m/z: 376.3 (M+1).

1. customPrepared similarly to that
2. customPurification by rpHPLC (Phenomenex Gemini C18, 10 μm, 150×30 mm; 10-100% ACN/water with 0.1% TFA)