تفاعل #42053

معادلة التفاعل

(R)-1-benzyl-3-(p-toluenesulfonyloxy)pyrrolidine

pyrrolidine

→

objective compound

المردود 69.8%

(S)-1-benzyl-3-(1-pyrrolidinyl)pyrrolidine

المردود 69.8%

المذيبات

ethanol

ظروف التفاعل

المعالجة

1. 1
   تركيزThe reaction solution was concentrated under reduced pressure
2. 2
   workup.ADDITIONmixed with water
3. 3
   استخلاصfollowed by extraction with ethyl acetate
4. 4
   تجفيفdried over anhydrous magnesium sulfate
5. 5
   workup.DISTILLATIONthe solvent was distilled off under reduced pressure
6. 6
   أخرىThe residue was purified by silica gel column chromatography

الإجراء التجريبي

2.00 g of (R)-1-benzyl-3-(p-toluenesulfonyloxy)pyrrolidine (J. Med. Chem., 1992, 35, 4205-4208) was dissolved in 12 ml of ethanol, 1.63 g of pyrrolidine was added, and then the mixture was stirred at 140° C. for 20 hours in a sealed tube. The reaction solution was concentrated under reduced pressure, mixed with water, followed by extraction with ethyl acetate, and dried over anhydrous magnesium sulfate, and then the solvent was distilled off under reduced pressure. The residue was purified by silica gel column chromatography to obtain 0.97 g of the objective compound as a brown oily product.

المصدر