反应详情

Following general procedure A-2, tert-butyl trans-4-[3-(cyclopropanecarbonyl)-6-(4-hydroxy-3-methoxyphenyl)quinolin-4-ylamino]cyclohexylcarbamate (45 mg, 0.085 mmol) was reacted with TFA (2 mL) to afford the desired product (11.3 mg, 31%) as a yellow solid: 1H NMR (500 MHz, CD3OD) δ 9.12 (s, 1H), 8.36 (s, 1H), 8.04-7.98 (m, 1H), 7.89 (d, J=8.7 Hz, 1H), 7.26 (d, J=1.9 Hz, 1H), 7.17 (dd, J=8.2, 2.0 Hz, 1H), 6.93 (d, J=8.2 Hz, 1H), 4.14 (s, 1H), 3.97 (s, 3H), 3.20-3.07 (m, 2H), 2.87-2.75 (m, 2H), 2.28 (d, J=12.2 Hz, 2H), 2.01 (d, J=11.6 Hz, 2H), 1.64-1.53 (m, 2H), 1.40-1.26 (m, 3H), 1.21-1.14 (m, 2H), 1.12-1.03 (m, 2H); ESI MS m/z 432 [C26H29N3O3+H]+; HPLC 98.8% (AUC), tR=7.95 min.