反应详情

tert-Butyl 4-{5-[4-({(4S,5R)-5-[3,5-bis(trifluoromethyl)phenyl]-4-methyl-2-oxo-1,3-oxazolidin-3-yl}methyl)-2-(3,3-difluoroazetidin-1-yl)pyrimidin-5-yl]-6-methoxypyridin-3-yl}-3-methylbenzoate (Step A, 639 mg, 0.805 mmol) was treated with 20 mL of a mixture of dichloromethane and trifluoroacetic acid (2 to 1 by volume) at room temperature for 0.5 hour, and purified on reverse phase HPLC to give the title compound as a white solid, after lyophilization. LCMS (M+H)+: 738.0. 1H NMR (CD3OD, 500 MHz): δ 8.26 (s, 1H), 8.22 (d, J=2.0 Hz, 1H), 8.00 (s, 1H), 7.96 (s, 1H), 7.93 (s, 2H), 7.90 (dd, J=1.5 Hz, 8.0 Hz, 1H), 7.71 (d, J=2.5 Hz, 1H), 7.38 (d, J=8.0 Hz, 1H), 5.87 (d, J=9.0 Hz, 1H), 4.69 (d, J=16.0 Hz, 1H), 4.45 (m, 4H), 4.43 (m, 1H), 4.15 (d, J=16.0 Hz, 1H), 4.00 (s, 3H), 2.38 (s, 3H), 0.73 (d, J=6.5 Hz, 3H). RTA IC50: 9 nM

1. custompurified on reverse phase HPLC