反应详情

A suspension of 4-chloro-6-cyano-7-(3-(1,1-dioxothiomorpholino)propoxy)quinoline (100 mg, 0.26 mmol), (prepared as described for the starting material in Example 1), 5-hydroxy-2-methylindole (46 mg, 0.32 mmol) and cesium carbonate (129 mg, 0.39 mmol) in DMF (1 ml) was stirred for 10 minutes at ambient temperature followed by 1.5 hours at 70° C. After cooling, water (5 ml) was added. The mixture was extracted with ethyl acetate. The organic layer was separated, washed with water, brine, dried (MgSO4) and evaporated. The residue was purified by column chromatography eluting with methanol/methylene chloride/ethyl acetate (5/45/50) to give 6cyano-7-(3-(1,1-dioxothiomorpholino)propoxy)-4-(2-methylindol-5-yloxy)quinoline (30 mg, 23%).

1. custom(prepared
2. waitfollowed by 1.5 hours at 70° C
3. temperatureAfter cooling
4. extractionThe mixture was extracted with ethyl acetate
5. customThe organic layer was separated
6. washwashed with water, brine
7. dry with materialdried (MgSO4)
8. customevaporated
9. customThe residue was purified by column chromatography
10. washeluting with methanol/methylene chloride/ethyl acetate (5/45/50)