反应详情

0.76 mL (5.49 mmol) of triethylamine and then 0.43 mL (5.49 mmol) of mesyl chloride are added to a solution of 1.52 g (4.99 mmol) of tert-butyl 2-hydroxy-6-azaspiro[3.4]octane-6-carboxylate, obtained in step 6.1., in 45 mL of dichloromethane. The reaction medium is stirred at room temperature for 1 hour 30 minutes. After evaporating off the solvent, water is added to the reaction medium, the aqueous phase is separated out and extracted several times with dichloromethane, the combined organic phases are washed with saturated aqueous sodium chloride solution and dried over sodium sulfate, and the filtrate is concentrated under reduced pressure. After evaporating off the solvent, 1.90 g of product are obtained in the form of a brown oil, which is used without further purification in the following step.

1. customobtained in step 6.1
2. customAfter evaporating off the solvent, water
3. additionis added to the reaction medium
4. customthe aqueous phase is separated out
5. extractionextracted several times with dichloromethane
6. washthe combined organic phases are washed with saturated aqueous sodium chloride solution
7. dry with materialdried over sodium sulfate
8. concentrationthe filtrate is concentrated under reduced pressure
9. customAfter evaporating off the solvent, 1.90 g of product
10. customare obtained in the form of a brown oil, which
11. customis used without further purification in the following step