反应详情

Following general procedure A-2, tert-butyl trans-4-[3-acetyl-6-(3-chloro-4-hydroxy-5-methoxyphenyl)quinolin-4-ylamino]cyclohexylcarbamate (35 mg, 0.065 mmol) was reacted with TFA (2 mL) to afford the desired product (13.6 mg, 48%) as an orange solid: 1H NMR (500 MHz, CD3OD) δ 8.95 (s, 1H), 8.32 (d, J=1.8 Hz, 1H), 8.04 (dd, J=8.7, 1.9 Hz, 1H), 7.92 (d, J=8.7 Hz, 1H), 7.27 (d, J=2.1 Hz, 1H), 7.22 (d, J=2.0 Hz, 1H), 4.23 (t, J=11.1 Hz, 1H), 3.99 (s, 3H), 3.24-3.16 (m, 1H), 2.70 (s, J=6.3 Hz, 3H), 2.41 (d, J=12.4 Hz, 2H), 2.18 (d, J=12.1 Hz, 2H), 1.80-1.66 (m, 2H), 1.61-1.50 (m, 2H); ESI MS m/z 440 [C24H26ClN3O3+H]+; HPLC 97.6% (AUC), tR=8.45 min.