Example 46
A mixture of compound 46-1 (15 mg, 0.03 mmol, 1 eq) and m-CPBA (16.0 mg, 0.07 mmol, 2 eq) in DCM (2 mL) was stirred at 25° C. for 1 hr. LC-MS showed the desired compound was detected. The reaction mixture was diluted with H2O (6 mL) and the mixture was extracted with EA (8 mL*3). The combined organic phase was washed with brine (8 mL*2), dried with anhydrous Na2SO4, filtered and concentrated in vacuum. The residue was purified by prep-HPLC. The title compound (7 mg, 15.9 umol, 42.8% yield) was obtained as white solid. LCMS (ESI): RT=0.828 min, mass calc. for C22H20F3NO3S 435.46, m/z found 436.0 [M+H]+; 1H NMR (400 MHz, CD3OD) δ 1.31-1.34 (m, 1H) 1.32-1.32 (m, 1H) 1.32-1.32 (m, 1H) 3.29 (s, 3H) 4.24-4.33 (m, 1H) 7.77 (d, J=8.03 Hz, 2H) 7.92 (d, J=8.03 Hz, 2H) 7.97 (d, J=8.78 Hz, 1H) 8.01 (d, J=1.76 Hz, 1H) 8.10 (dd, J=8.78, 1.76 Hz, 1H) 8.55 (br d, J=7.28 Hz, 1H) 8.67 (d, J=1.51 Hz, 1H) 8.75 (s, 1H).
