反应详情

A solution of the 3-(4-[2-(2-biphenyl-4-yl-5-methyl-oxazol-4-yl)-ethoxy]-2-{[(2,5-dichloro-thiophene-3-carbonyl)-amino]-methyl}-phenyl)-propionic acid tert-butyl ester (367 mg, 0.531 mmol) in CH2Cl2 (20 mL) was treated with anisole (2.0 mL) then TFA (6.0 mL). The mixture was stirred at room temperature for 2 h and concentrated. The residue was co-evaporated with CCl4 three times, dried under vacuum, triturated with ether, and filtered to obtain the title compound as a white solid (301 mg, 73%). 1H NMR (400 MHz, DMSO-d6): δ 2.25 (s, 3H), 2.38 (t, 2H, J=8.3 Hz), 2.71 (t, 2H, J=7.3 Hz), 2.82 (t, 2H, J=6.3 Hz), 4.07 (t, 2H, J=6.6 Hz), 4.28 (d, 2H, J=4.9 Hz), 6.68 (d, 1H, J=9.3 Hz), 6.77 (s, 1H), 7.00 (d, 1H, J=8.3 Hz), 7.24 (s, 1H), 7.29 (t, 1H, J=5.9 Hz), 7.39 (t, 2H, J=7.8 Hz), 7.63 (t, 2H, J=7.8 Hz), 7.71 (d, 2H, J=8.3 Hz), 7.88 (d, 2H, J=8.3 Hz), 8.69 (t, 2H, J=5.9 Hz). MS (ES) m/e 635.1 [M+1].

1. concentrationconcentrated
2. customdried under vacuum
3. customtriturated with ether
4. filtrationfiltered