反应详情

400 mg of 2-[3-(6-Fluoro-1-tert-butoxycarbonyl-1H-indazol-3-ylmethyl)-2,4-dioxo-5-phenyl-2,3,4,5-tetrahydro-benzo[b][1,4]diazepin-1-yl)-N-isopropyl-N-phenyl-acetamide, prepared as in Intermediate 69, is dissolved in 10 mL of CHCl3 and 5 mL of TFA is added. The reaction mixture is stirred for 6 h and the solvents were removed in vacuo to afford 240 mg of the title compound: 1H NMR (400 MHz, DMSO-d6) δ7.82-6.88 (m, 18H), 4.77(m, 1H, J=6.8), 4.45 (d, 1H, J=16.8), 4.12 (m, 2H), 3.41 (m, 2H), 0.95 (t, 6H, J=6.8); low resolution MS (FAB) m/e 576 (MH+); Tr =10.31 min. (HPLC Column: Dynamax C-8 2 mL/min., 50-90% Acetonitrile in aqueous TFA (0.1% v/v) over 15 min.).

1. customthe solvents were removed in vacuo