(2-(Difluoromethyl)phenyl)boronic acid → 5-amino-N-(5-((2S,5R,6S)-5-amino-6-fluorooxepan-2-yl)-1-methyl-1H-pyrazol-4-yl)-2-(2-(difluoromethyl)phenyl)thiazole-4-carboxamide

Beteiligte Stoffe

Reaktionsschritte

Following the procedure for Example 101 starting from tert-butyl N-[2-bromo-4-[[5-[(2S,5R,6S)-5-(tert-butoxycarbonylamino)-6-fluoro-oxepan-2-yl]-1-methyl-pyrazol-4-yl]carbamoyl]thiazol-5-yl]carbamate (Intermediate 95), and replacing 3,6-dihydro-2H-pyran-4-boronic acid pinacol ester with (2-(difluoromethyl)phenyl)boronic acid gave 335. 1H NMR (400 MHz, DMSO-d6) δ 9.05 (s, 1H), 8.09-7.80 (m, 1H), 7.77 (d, J=7.6 Hz, 1H), 7.71-7.66 (m, 2H), 7.65-7.59 (m, 1H), 7.59-7.50 (m, 3H), 4.75 (dd, J=10.6, 3.8 Hz, 1H), 4.42-4.26 (m, 1H), 4.19-4.07 (m, 1H), 4.04-3.87 (m, 1H), 3.79 (s, 3H), 3.21-3.08 (m, 1H), 2.08-1.99 (m, 1H), 1.97-1.85 (m, 1H), 1.74-1.58 (m, 4H). LCMS (ES+) m/z 481 (M+1).

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