反应详情

Following the general procedure outlined in Synthetic Scheme VI, 2.56 g (7.37 mmol) of 1-bromo-4,5-difluoro-2-[(4-methylsulfonyl)phenyl]benzene (Example 18, Step 2) was reacted with 1.35 g (9.93 mmol) of 4-methylphenylboronic acid. Purification by silica gel chromatography (MPLC) with ethyl acetate/hexane (3:7) gave 2.55 g (97%) of 1,2-difluoro-4-(4-methylphenyl)-5-[4-(methylsulfonyl)phenyl]benzene as a colorless solid: mp 147.0-148.0° C.; NMR (CDCl3) δ 2.32 (s, 3H), 3.05 (s, 3H), 6.92 (d, J=8 Hz, 2H), 7.03 (d, J=8 Hz, 2H), 7.17-7.32 (m, 4H), 7.79 (d, J=8 Hz, 2H). MS (FAB): m/e 365 (M+Li). Anal. Calc'd for C20H16F2O2S: C, 67.03; H, 4.50. Found: C, 67.18; H, 4.48.

1. customPurification by silica gel chromatography (MPLC) with ethyl acetate/hexane (3:7)