反应详情

Following a procedure analogous to that for the synthesis of Intermediate 1F, ethyl 2-(4-(N-butyl-4-chloro-5-methyl-1-(4-(naphthalen-2-ylsulfonylcarbamoyl)-2-(1,2,3,4-tetrahydroisoquinoline-2-carbonyl)phenyl)-1H-pyrazole-3-carboxamido)phenyl)acetate (Example 155, 1 mg, 9.9 μmol) was converted to the title compound (0.5 mg, 53%). 1H NMR (CD3OD, 2:1 mixture of amide rotamers) δ 8.71 (s, 1H), 8.10 (d, J=9.2 Hz, 1H), 8.06 (s, 2H), 8.03-7.97 (m, 2.5H), 7.94-7.91 (m, 0.5H), 7.73-7.65 (m, 2H), 7.41 (br s, 0.5H), 7.30 (br s, 0.5H), 7.23-7.10 (m, 5H), 7.03-6.96 (m, 1H), 6.90 (d, J=8.4 Hz, 1H), 6.61 (br s, 1H), 4.73 (br s, 1H), 4.48-4.19 (m, 2H), 4.07 (br s, 1H), 3.91 (br s, 1H), 3.54-3.39 (m, 2H), 2.95-2.75 (m, 2H), 2.10 (s, 2H), 2.01 (s, 1H), 1.65-1.55 (m, 1H), 1.40-1.18 (m, 5H), 0.92-0.80 (m, 3H); MS(ESI+) m/z 818.3 (M+H)+.