Benzylamine → (S)-2-Benzylcarbamoyl-pyrrolidine-1-carboxylic acid benzyl ester

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Reaction Steps

To a solution of 5.00 g Z-Pro-OH in 50 ml DMF were added 3.84 g EDC, 2.73 g HOAt, 7.3 ml DIPEA and 2.2 ml benzylamine at 0° C. After stirring for 2 h the reaction mixture was concentrated, the residue was dissolved in dichloromethane and subsequently extracted with aqueous LiCl (4%), 0.1 M HCl and saturated NaHCO3. The crude product obtained after evaporation of the solvent was pure enough for the subsequent transformation. Yield: 7.11 g colorless amorphous solid.

Provenance & Evidence