反应详情

The bromo-derivative (84) (100 mg, 0.29 mmol) was coupled to 4-chloro-phenylboronic acid (49 mg, 0.32 mmol) using Method E. After reaction, the solvents were removed under a stream of N2, and the residue was dissolved in saturated NaHCO3 solution (5 ml) and washed with EtOAc (5 ml). The aqueous layer was acidified to pH 1 with 2M HCl until a white precipitate formed and extracted with EtOAc (2×5 ml). The organic layer was dried (MgSO4), filtered and the solvent removed in vacuo. The residue was triturated with MeCN (4 ml) and further purified by preparative HPLC to give the title compound.

1. customAfter reaction
2. customthe solvents were removed under a stream of N2
3. dissolutionthe residue was dissolved in saturated NaHCO3 solution (5 ml)
4. washwashed with EtOAc (5 ml)
5. customformed
6. extractionextracted with EtOAc (2×5 ml)
7. dry with materialThe organic layer was dried (MgSO4)
8. filtrationfiltered
9. customthe solvent removed in vacuo
10. customThe residue was triturated with MeCN (4 ml)
11. customfurther purified by preparative HPLC