反应详情

To a solution of 2-(2-naphthyloxy)acetic acid (1.1 g, 5.0 mmol) in anhydrous tetrahydrofuran (25 ml) carbonyl-diimidazole (0.80 g, 5.0 mmol) was added in portions, under stirring at room temperature. After 15 minutes a solution of 1-[2,6-di(1-pyrrolidinyl)-4-pyrimidinyl]homopiperazine (1.58 g, 5.0 mmol) in anhydrous tetrahydrofuran (15 ml) was added dropwise. The mixture was stirred at room temperature for 8 hours and the solvent was distilled off under reduced pressure. The residue was dissolved in methylene chloride, the solution was washed three times with water, dried over MgSO4 and concentrated. The obtained crude product was chromatographed over a silica gel column eluting with a 1:2 mixture of benzene and ethyl acetate to afford 0.7 g of the title compound, yield: 28%, mp. 103°-110° C.

1. stirringThe mixture was stirred at room temperature for 8 hours
2. distillationthe solvent was distilled off under reduced pressure
3. dissolutionThe residue was dissolved in methylene chloride
4. washthe solution was washed three times with water
5. dry with materialdried over MgSO4
6. concentrationconcentrated
7. customThe obtained crude product
8. customwas chromatographed over a silica gel column
9. washeluting with a 1:2 mixture of benzene and ethyl acetate