反应详情

To 12 mg of tert-butyl (1S,2R)-1-{[(S)-tert-butylsulfinyl]amino}-7-fluoroindane-2-carboxylate (compound of Preparation Example 113a) was added 0.4 ml of a 10% hydrogen chloride/methanol solution, followed by stirring for 1 hour under ice-cooling. To the reaction mixture was added 1 ml of a 10% hydrogen chloride/methanol solution, followed by stirring at 50° C. for 6 hours. After leaving to be cooled, the solvent was evaporated under reduced pressure, and then to the obtained residue were added a saturated aqueous sodium hydrogen carbonate solution and ethyl acetate to carry out a layer separation operation. The organic layer was washed with saturated brine and dried over anhydrous magnesium sulfate, and the solvent was evaporated under reduced pressure to obtain 6 mg of methyl (1S,2R)-1-amino-7-fluoroindane-2-carboxylate.

1. temperaturecooling
2. stirringby stirring at 50° C. for 6 hours
3. customAfter leaving
4. temperatureto be cooled
5. customthe solvent was evaporated under reduced pressure
6. additionto the obtained residue were added a saturated aqueous sodium hydrogen carbonate solution and ethyl acetate
7. customa layer separation operation
8. washThe organic layer was washed with saturated brine
9. dry with materialdried over anhydrous magnesium sulfate
10. customthe solvent was evaporated under reduced pressure