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In 13 ml of ethanol, 4.71 g of (S)-2-pyrrolidinemethanol was dissolved, followed by the addition of 4.6 ml of acrylonitrile. The resulting mixture was heated under reflux for 2 hours. After the solvent was evaporated, the residue was dissolved in 70 ml of toluene, followed by the addition of 13 ml of triethylamine under ice-cooling. To the resulting mixture, 4.3 ml of methanesulfonyl chloride was added dropwise, followed by stirring at 0° C. for 10 minutes and then at room temperature for 30 minutes. After the addition of 15.7 g of potassium tert-butoxide, the mixture was stirred at room temperature for 16 hours. Water was added to the reaction mixture, and the toluene layer was separated and dried over anhydrous sodium sulfate. The solvent was evaporated and the resulting residue was subjected to silica gel column chromatography, whereby 5.22 g of (5S)-1-azabicyclo[3.3.0]octane-3-carbonitrile was obtained as a diastereomer mixture from the fraction eluted with chloroform-methanol-29% aqueous ammonia (100:10:1).

1. temperatureThe resulting mixture was heated
2. temperatureunder reflux for 2 hours
3. customAfter the solvent was evaporated
4. dissolutionthe residue was dissolved in 70 ml of toluene
5. additionfollowed by the addition of 13 ml of triethylamine under ice-
6. temperaturecooling
7. additionTo the resulting mixture, 4.3 ml of methanesulfonyl chloride was added dropwise
8. waitat room temperature for 30 minutes
9. additionAfter the addition of 15.7 g of potassium tert-butoxide
10. stirringthe mixture was stirred at room temperature for 16 hours
11. additionWater was added to the reaction mixture
12. customthe toluene layer was separated
13. dry with materialdried over anhydrous sodium sulfate
14. customThe solvent was evaporated