反应详情

(Method 2) To the THF (5.6 ml) solution of 2-[1-(6-cyano-1-methanesulfonyl-1H-indol-2-yl)-1-methylethyl]-4-methoxy-benzoic acid methyl ester (Compound AA4, 138 mg, 0.324 mmol), tetrabutylammonium fluoride (514 mg, 6 eq.) was added, and the mixture was stirred at room temperature overnight. Thereafter, 2 M aqueous solution of sodium hydroxide (5.6 ml) was added to the mixture, which was then stirred for 4 hr, added with 1 M HCl, and extracted with ethyl acetate. The organic layer was washed with brine and dried over magnesium sulfate. The drying agent was removed by filtration and the residues obtained after concentration under reduced pressure were dissolved in ethyl acetate (10 ml) and added with e 4 M HCl and ethyl acetate solution (10 ml) followed by stirring at room temperature for 30 min. The residues obtained after concentration of the reaction solution under reduced pressure were purified by silica gel column chromatography (ethyl acetate/hexane) to obtain the title compound (89.2 mg, 62%).

1. stirringwas then stirred for 4 hr
2. extractionextracted with ethyl acetate
3. washThe organic layer was washed with brine
4. dry with materialdried over magnesium sulfate
5. customThe drying agent was removed by filtration
6. customthe residues obtained
7. concentrationafter concentration under reduced pressure
8. dissolutionwere dissolved in ethyl acetate (10 ml)
9. additionadded with e 4 M HCl and ethyl acetate solution (10 ml)
10. stirringby stirring at room temperature for 30 min
11. customThe residues obtained after concentration of the reaction solution under reduced pressure
12. customwere purified by silica gel column chromatography (ethyl acetate/hexane)