反应详情

(1S)-2,2-Dimethyl-1-({3-[4-(trifluoromethyl)phenyl]-1H-pyrazol-1-yl}methyl)propyl (1S)-1-{[(4-morpholinylcarbonyl)amino]acetyl}pentylcarbamate was prepared (50% yield) as in example 3g except that (1S)-2,2-dimethyl-1-({3-[4-(trifluoromethyl)phenyl]-1H-pyrazol-1-yl}methyl)propyl (1S)-1-{(1 S)-1-hydroxy-2-[(4-morpholinylcarbonyl)amino]ethyl}pentylcarbamate & (1S)-2,2-dimethyl-1-({3-[4-(trifluoromethyl)phenyl]-1H-pyrazol-1-yl}methyl)propyl (1S)-1-{(1R)-1-hydroxy-2-[(4-morpholinylcarbonyl)amino]ethyl}pentylcarbamate were substituted for (1S)-2,2-dimethyl-1-({3-[4-(trifluoromethyl)phenyl]-1H-pyrazol-1-yl}methyl)propyl (1S)-1-{(1S)-1-hydroxy-2-[(2-pyridinylsulfonyl)amino]ethyl}pentylcarbamate & (1S)-2,2-dimethyl-1-({3-[4-(trifluoromethyl)phenyl]-1H-pyrazol-1-yl}methyl)propyl (1S)-1-{(1R)-1-hydroxy-2-[(2-pyridinylsulfonyl)amino]ethyl}pentylcarbamate. 1H-NMR (300 MHz, DMSO-d6): δ 8.00 (d, J=8 Hz, 2H), 7.74 (m, 3H), 7.47 (d, J=8 Hz, 1H), 6.81–6.72 (m, 2H), 4.87 (d, J=9 Hz, 1H), 4.48 (m, 1H), 4.22 (m, 1H), 3.88-3.75 (m, 2H), 3.53 (t, J=4 Hz, 4H), 3.38 under water peak (m, 1H), 3.24 (t, J=4 Hz, 4H), 1.55 (m, 1H), 1.33 (m, 1H), 1.15–0.85 (m, 13H), 0.72 (t, J=6 Hz, 3H); ES-LCMS m/z 596 (M+H); HRMS C29H40N5O5F3 m/Z 596.3060 (M+H)+Cal; 596.3047 (M+H)+.