反应详情

The title compound was prepared from 5-cyclohexyl-1,3-dihydro-1-propyl-3(R,S)-[(4-nitrophenyloxycarbonyl)amino]-2H-1,4-benzodiazepin-2-one (0.3 g, 0.65 mmol), triethylamine (90 μl, 0.65 mmol), dimethylformamide (6 ml) and 1-(methylsulphonylaminocarbonyl)-3-aminobenzene ( 0.15 g, 7.1 mmol) [Example 16, Step 2] using the procedure described in Example 11, Step 4. The product (0.16 g, 46%) was afforded as a cream solid after trituration with hot methanol. mp 205° C. (dec.). 1H NMR (360 MHz, D6 -DMSO) δ 0.73 (3H, t, J=7.3 Hz), 0.86-1.00 (1H, m), 1.08-1.42 (5H, m), 1.43-1.54 (2H, m), 1.57-1.67 (2H, m), 1.74-1.83 (1H, m), 1.87-1.96 (1H, m), 2.91-3.01 (1H, m), 3.33 (3H, s), 3.62-3.72 (1H, m), 4.16-4.26 (1H, m), 5.04 (1H, d, J=7.8 Hz), 7.34-7.43 (3H, m), 7.47 (1H, d, 7.8 Hz), 7.56-7.68 (3H, m), 7.77 (1H, d, J=7.7 Hz), 7.91 (1H, dd, J=1.9 and 1.9 Hz), 9.20 (1H, s), 12.04 (1H, brs).