反应详情

A solution of 0.52 g (2.3 mmol) of (R/S)-1-benzyl-pyrrolidin-3-yl carboxylic acid, methyl ester (from Step A) in 5 mL of 1,2-dichloroethane was treated with 0.3 mL (2.7 mmol) of 1-chloroethyl chloroformate (ACE-Cl). The resulting mixture was stirred at rt for 3 h, then at reflux for 30 min. The reaction was cooled and concentrated. The residue was warmed to reflux in 5 mL of MeOH for 1 h. The reaction was cooled and concentrated. The crude product was used in Step C without further purification.

1. temperatureat reflux for 30 min
2. temperatureThe reaction was cooled
3. concentrationconcentrated
4. temperatureThe residue was warmed
5. temperatureto reflux in 5 mL of MeOH for 1 h
6. temperatureThe reaction was cooled
7. concentrationconcentrated
8. customThe crude product was used in Step C without further purification