Cyclobutylamine → (S)-2-Cyclobutylcarbamoyl-pyrrolidine-1-carboxylic acid benzyl ester

Participants

Reaction Steps

To a solution of 5.00 g pyrrolidine-1,2-dicarboxylic acid 1-benzyl ester in 100 ml DMF were added 2.73 g HOAt, 3.85 g EDC, 6.9 ml DIPEA and 1.43 g cyclobutylamine. After 24 h the mixture was diluted with ethyl acetate and subsequently extracted with aqueous LiCl (4% w/w), 0.1 M HCl and saturated aqueous NaHCO3. The organic layer was dried over MgSO4 and the solvent was removed under reduced pressure to give the crude which was pure enough for the subsequent transformation. Yield: 9.00 g.

Provenance & Evidence