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Updated: Jan 3, 2026

Preparation of Contiguous Bisaziridines for Regioselective Ring-Opening Reactions
Published on: July 28, 2022
Enantioselective Aza-Reformatsky Reaction with Ketimines
Aitor Maestro1, Edorta Martinez de Marigorta1, Francisco Palacios1
1Departamento de Química Orgánica I , Facultad de Farmacia, University of the Basque Country , UPV/EHU Paseo de la Universidad 7 , 01006 Vitoria-Gasteiz , Spain.
Abstract:
Here, an enantioselective aza-Reformatsky reaction using acyclic ketimine substrates is presented. Using α-phosphorated ketimines as electrophilic substrates and a simple BINOL-derived ligand, phosphorated analogues of aspartic acid holding chiral tetrasubstituted carbons are efficiently obtained with excellent enantioselectivity through an asymmetric organocatalytic Reformatsky-type reaction. The phosphorated analogues of aspartic acid have been used for the synthesis of phosphorus-containing enantiopure tetrasubstituted β-lactams.
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