反应详情

A solution of N1-[1-(4-pyridyl)piperidin-4-ylmethyl]-1,2-benzenediamine (212 mg, 0.75 mmol) and pyridine (4 mL) in chloroform (2 mL) at 0° C. was treated with a solution of 4-methoxybenzoyl chloride (128 mg, 0.75 mmol) in chloroform. The mixture was allowed to warm to room temperature and stir for 17 h. The mixture was concentrated and the residue was dissolved in EtOAc. The organic layer was washed with 1 N NaOH (2×), water (3×), brine (1×), dried (K2CO3), and concentrated. The residue was purified by RPHPLC, yielding 52 mg (17%) of the title compound as a hydrochloride salt.

1. concentrationThe mixture was concentrated
2. dissolutionthe residue was dissolved in EtOAc
3. washThe organic layer was washed with 1 N NaOH (2×), water (3×), brine (1×)
4. dry with materialdried (K2CO3)
5. concentrationconcentrated
6. customThe residue was purified by RPHPLC