反应详情

3-((3S,4S)-3-Fluoro-tetrahydro-pyran-4-ylamino)-isoquinoline-6-carboxylic acid [(S)-1-(4-chloro-3-fluoro-phenyl)-2-hydroxy-ethyl]-amide (II-54) was prepared analogously except in step 2, (S)-2-aminopropan-1-ol was replaced with (3S,4S)-3-fluorotetrahydro-2H-pyran-4-amine (71c) and in step 5, 50c was replaced with (S)-2-amino-2-(4-chloro-3-fluoro-phenyl)ethanol hydrochloride (62e). 1H NMR (500 MHz, MeOH-d4): δ 8.90 (s, 1H), 8.09 (s, 1H), 7.92-7.88 (m, 1H), 7.61-7.59 (m, 1H), 7.47-7.45 (m, 1H), 7.38-7.33 (m, 1H), 7.28-7.24 (m, 1H), 6.91 (d, J=9.0 Hz, 1H), 5.21 (t, J=6.5 Hz, 1H), 4.84-4.73 (m, 1H), 4.27-4.11 (m, 2H), 4.05-4.02 (m, 1H), 3.92-3.80 (m, 2H), 3.75-3.60 (m, 2H), 2.06-1.96 (m, 1H), 1.93-1.88 (m, 1H).