反应详情

2-Butyl-4-chloro-1-[[1-(2-cyanophenyl)-1H-indol-4-yl]methyl]-1H-imidazole-5-carboxylic acid (910 mg, 2.1 mmol, prepared as described in part C of Example 9), the title B compound (930 mg, 7.6 mmol), sodium iodide (795 mg, 5.03 mmol), cesium carbonate (2.6 g, 7.98 mmol) and dimethylformamide (4.0 mL) were combined and were stirred at room temperature for 16 hours. The reaction was diluted with ethyl acetate and filtered. The organic phase was washed with pH=4 buffer twice, pH 7 buffer once, saturated sodium chloride once, dried over anhydrous magnesium sulfate, filtered and concentrated to give a yellow oil. Purification by chromatography on Merck silica gel (250 g) eluting with (8:2) hexane/ethyl acetate gave the title B compound (1.06 g).

1. filtrationfiltered
2. washThe organic phase was washed with pH=4 buffer twice
3. dry with materialpH 7 buffer once, saturated sodium chloride once, dried over anhydrous magnesium sulfate
4. filtrationfiltered
5. concentrationconcentrated
6. customto give a yellow oil
7. customPurification by chromatography on Merck silica gel (250 g)
8. washeluting with (8:2) hexane/ethyl acetate