反应详情

To N-(2-(2-amino-3-benzyl-6-fluoro-2,3-dihydro-1H-inden-5-yloxy)ethyl)-1-methyl-1H-imidazole-4-sulfonamide (17.9 mg, 0.040 mmol) was added 1,3-dibromopropane (4.904, 0.048 mmol) and potassium carbonate (6.12 mg, 0.044 mmol) in water (1 mL)+5 drop acetonitrile were added. Microwave at 120° C. for 20 min. Evaporated acetonitrile, re-dissolved in dichloromethane and extracted with water and brine, dried over sodium bicarbonate, filtered and evaporated to obtain the crude product, that was purified by flash silica gel chromatography on 4 g SiO2-cartridge using 10% methanol in dichloromethane to afford cis-N-(2-{[2-(azetidin-1-yl)-3-benzyl-6-fluoro-2,3-dihydro-1H-inden-5-yl]oxy}ethyl)-1-methyl-1H-imidazole-4-sulfonamide as a clear glass. m=4.0 mg (20%)

1. additionwere added
2. extractionextracted with water and brine
3. dry with materialdried over sodium bicarbonate
4. filtrationfiltered
5. customevaporated
6. customto obtain the crude product, that
7. customwas purified by flash silica gel chromatography on 4 g SiO2-cartridge