反应详情

4-Methyl-3-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)-benzoic acid (Intermediate 4) (2 g) was dissolved in DMF (20 ml). To this was added 3-methoxyaniline (0.985 g), DIPEA (4 ml) and HATU (3.05 g). The mixture was stirred for 18 h at room temp. The solvent was removed under vacuum and the residue was partitioned between ethyl acetate (250 ml) and water (50 ml). The organic layer was dried (magnesium sulphate) concentrated under vacuum and purified using a silica Biotage cartridge (90 g) eluting with 1:4 ethyl acetate/cyclohexane to give the title compound as a white solid (2.06 g).

1. customThe solvent was removed under vacuum
2. customthe residue was partitioned between ethyl acetate (250 ml) and water (50 ml)
3. dry with materialThe organic layer was dried (magnesium sulphate)
4. concentrationconcentrated under vacuum
5. custompurified
6. washeluting with 1:4 ethyl acetate/cyclohexane