反应详情

The title product was prepared according to the procedure of Example 112, Step 3, starting from tert-butyl 4-[(5-amino-1-benzofuran-7-yl)methyl]-3-methylpiperazine-1-carboxylate (45 mg crude material, 0.10 mmol; obtained in Example 112, Step 2) and 2,5-dichlorothiophene-3-sulphonyl chloride (38 mg, 0.15 mmol). The title compound (23 mg, 43%) was obtained as an off-white solid. HPLC 98%, RT=1.61 min (System A; 10-97% MeCN over 3 min), 100%, RT=1.43 min (System B; 10-100% MeCN over 3 min). 1H NMR (400 MHz, methanol-d4) δ ppm 1.53 (d, J=6.27 Hz, 3H) 2.87-3.02 (m, 1H) 3.14-3.27 (m, 2H) 3.39-3.47 (m, 1H) 3.47-3.54 (m, 1H) 4.12-4.24 (m, 1H) 4.62-4.71 (m, 1H) 6.89 (d, J=2.26 Hz, 1H) 7.13 (s, 1H) 7.30-7.32 (m, J=1.76 Hz, 1H) 7.45 (d, J=2.26 Hz, 1H) 7.85 (d, J=2.26 Hz, 1H). *Two hydrogens are not visible in the spectrum. Probably “hidden” behind the H2O— and the MeOH signals. MS (ESI+) for C18H19Cl2N3O3S2 m/z 460 (M+H)+.

1. customThe title product was prepared