反应详情

Following a procedure analogous to that for the synthesis of Example 125, 4-chloro-5-methyl-1-(4-(naphthalen-2-ylsulfonylcarbamoyl)-2-(1,2,3,4-tetrahydroisoquinoline-2-carbonyl)phenyl)-1H-pyrazole-3-carboxylic acid (Intermediate 122F, 25 mg, 0.040 mmol) and N-benzylbutan-1-amine (Aldrich, 11 μL, 0.064 mmol) were converted to the title compound (21 mg, 68%). 1H NMR (1:1 CD3OD:CDCl3) δ 8.62 (br s, 1H), 8.15 (d, J=7.9 Hz, 1H), 8.07-7.82 (m, 5H), 7.64-7.50 (m, 1H), 7.46-7.36 (m, 1.5H), 7.28-6.93 (m, 9H), 6.86 (d, J=7.3 Hz, 0.5H), 4.62 (d, J=5.9 Hz, 1H), 4.47-4.11 (m, 2.5H), 3.77-3.36 (m, 2.5H), 3.21-2.94 (m, 1.5H), 2.81-2.65 (m, 2.5H), 2.35-2.14 (m, 3H), 1.74-1.13 (m, 3H), 1.08-0.77 (m, 3H), 0.72-0.58 (m, 1H); MS(ESI+) m/z 774.1 (M+H)+.