反应详情

A solution of Example 122E (411 mg, 1 mmol), 2M dimethylamine in THF (1 mL), EDCI (296 mg, 1.5 mmol), and DMAP (10 mg) in DMF (10 mL) at room temperature was stirred for 16 hours, diluted with ethyl acetate (200 mL), washed sequentially with 1N HCl (50 mL), water (50 mL), and brine (20 mL), dried (MgSO4), filtered, and concentrated. The concentrate was purified by flash column chromatography on silica gel with 100% ethyl acetate to provide the desired product. MS (ESI(+)) m/e 439 (M+H)+.

1. washwashed sequentially with 1N HCl (50 mL), water (50 mL), and brine (20 mL)
2. dry with materialdried (MgSO4)
3. filtrationfiltered
4. concentrationconcentrated
5. customThe concentrate was purified by flash column chromatography on silica gel with 100% ethyl acetate