反应详情

3-(Tetrahydro-pyran-4-ylamino)-isoquinoline-6-carboxylic acid [(S)-(3-fluoro-phenyl)-(1-methyl-1H-pyrazol-4-yl)-methyl]-amide (II-9) was prepared analogously except in step 2, (S)-2-aminopropan-1-ol was replaced with 4-amino-tetrahydropyran and in step 5, 50c was replaced with (S)-(3-fluoro-phenyl)(1-methyl-1H-pyrazol-4-yl)methanamine hydrochloride (50h). 1H NMR (400 MHz, DMSO) δ 9.26 (d, J=8.5 Hz, 1H), 8.91 (s, 1H), 8.10 (s, 1H), 7.84 (d, J=8.6 Hz, 1H), 7.57 (s, 1H), 7.54 (dd, J=8.5, 1.4 Hz, 1H), 7.40 (td, J=8.0, 6.1 Hz, 1H), 7.36 (s, 1H), 7.30-7.24 (m, 2H), 7.09 (td, J=8.6, 2.5 Hz, 1H), 6.73 (s, 1H), 6.51 (d, J=8.0 Hz, 1H), 6.33 (d, J=8.5 Hz, 1H), 3.92-3.86 (m, 2H), 3.86-3.80 (m, 1H), 3.79 (s, 3H), 3.44 (td, J=11.8, 2.0 Hz, 2H), 1.92 (d, J=10.5 Hz, 2H), 1.49 (ddd, J=15.6, 12.0, 4.2 Hz, 2H).