反应详情

温度

60 °C

1.00 g of tert-butyl (6-hydroxy-2,3-dihydro-1H-inden-5-yl)carbamate was dissolved in 10.0 mL of DMF, and 1.08 g of ethyl 5-(bromomethyl)pyrazine-2-carboxylate and 721 mg of potassium carbonate were added thereto, followed by stirring at 60° C. for 1 hour. The reaction liquid was poured into a 5% w/v aqueous citric acid solution, followed by extraction with ethyl acetate. The organic layer was washed with a 5% w/v aqueous citric acid solution, water, and saturated brine, and then dried over anhydrous magnesium sulfate. The solvent was evaporated and the obtained residue was purified by silica gel column chromatography (hexane:ethyl acetate=9:1 to 7:3) to obtain 690 mg of ethyl 5-[({6-[(tert-butoxycarbonyl)amino]-2,3-dihydro-1H-inden-5-yl}oxy)methyl]pyrazine-2-carboxylate.

1. customThe reaction liquid
2. extractionfollowed by extraction with ethyl acetate
3. washThe organic layer was washed with a 5% w/v aqueous citric acid solution, water, and saturated brine
4. dry with materialdried over anhydrous magnesium sulfate
5. customThe solvent was evaporated
6. customthe obtained residue was purified by silica gel column chromatography (hexane:ethyl acetate=9:1 to 7:3)