反应详情

To a solution of (10) and a benzaldehyde (unsubstituted or substituted by R1) in DCM are added MgSO4, AcOH, and then NaBH3CN. The reaction mixture is stirred overnight, and then diluted with DCM. The organic solution is washed with NaHCO3, dried and concentrated. The residue is dissolved in water, treated with (Boc)2O, and then stirred overnight. The reaction mixture is extracted with DCM, dried, and concentrated to give product 1-benzyl-4-[tert-butoxycarbonyl-(benzyl)-amino]-pyrrolidine-2-carboxylic acid methyl ester (11).

1. washThe organic solution is washed with NaHCO3
2. customdried
3. concentrationconcentrated
4. dissolutionThe residue is dissolved in water
5. additiontreated with (Boc)2O
6. stirringstirred overnight
7. extractionThe reaction mixture is extracted with DCM
8. customdried
9. concentrationconcentrated