反应详情

tert-butyl[1-(4-{2-[4-(morpholin-4-ylmethyl)phenyl]-9H-imidazo[1,2-d]pyrido[2,3-b][1,4]benzodiazepin-3-yl}phenyl)cyclobutyl]carbamate (28 mg, 0.043 mmol) in MeOH (0.5 mL) was added 4N HCl-dioxane (2 mL) and stirred at r.t for 15 hours. The mixture was concentrated to afford the desired product (31 mg, quant) as a yellow solid. 1HNMR (DMSO-d6) 400 MHz δ: 8.74 (br s, 2H), 8.61 (s, 1H), 8.10 (dd, J=4.9 Hz and 1.4 Hz, 1H), 7.96 (dd, J=7.7 Hz and 1.4 Hz, 1H), 7.59 (dd, J=15.5 Hz and 8.6 Hz, 4H), 7.53 (d, J=8.6 Hz, 2H), 7.36 (d, J=7.4 Hz, 3H), 7.30 (dd, J=7.4 Hz and 1.1 Hz, 1H), 7.13 (td, J=7.4 Hz and 1.1 Hz, 1H), 6.88 (dd, J=8.0 Hz and 1.1 Hz, 1H), 6.73 (dd, J=7.4 Hz and 4.9 Hz, 1H), 5.76 (s, 2H), 4.30 (d, J=5.2 Hz, 2H), 3.94 (dd, J=12.0 Hz and 2.3 Hz, 2H), 3.22 (d, J=11.5 Hz, 2H), 3.11-3.04 (m, 2H), 2.59-2.55 (m, 4H), 2.24-2.16 (m, 1H), 1.87-1.78 (m, 1H). LCMS: 555 [M+H].

1. concentrationThe mixture was concentrated