反应详情

Starting from the amine 287, following the procedure described above for the synthesis of compound 269b (scheme 561, example 222) and replacing 2-(2,6-dichlorophenyl)acetyl isothiocyanate with 2-phenylacetyl isothiocyanate, title compound 288 was obtained in 72% yield as a yellowish solid. 1H NMR (d-DMSO) δ (ppm): 12.51 (s, 1H), 11.84 (s, 1H), 8.64(dd, 1H, J1=5.1 Hz, J2=0.4 Hz), 8.24 (s, 1H, J=0.4Hz), 8.02(dd, 1H, J1=1.8 Hz, J2=13.4 Hz), 7.56-7.54 (m, 2H), 7.36-7.31 (m, 1H), 7.28-7.25 (m, 1H), 6.81 (d, 1H, J=5.5 Hz), 3.91 (s, 3H), 3.81 (s, 2H). MS (m/z): 496.3 (M+H) (found).