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A new synthesis of β-amino acids by use of ketene diethyl acetal as enolate equivalent
Authors:Kai Rossen  Pavol Jakubec  Matthias Janik
Affiliation:a Degussa AG, EC-EX-R&D-WO, Rodenbacher Chaussee 4, 63457 Hanau, Germany
b Degussa AG, Aqura NMR Department, Rodenbacher Chaussee 4, 63457 Hanau, Germany
Abstract:Reaction of phenylsulfonyl formamides, readily available in a single step from an aromatic aldehyde and sodium phenylsulfinate, with ketene diethyl acetal under basic conditions gives N-formyl β-amino acid esters in good yield, which can be kinetically resolved with a lipase.
Keywords:β-Amino acid   Ketene diethylacetal   Acyl imine   Acetate enolate   Enzymic kinetic resolution
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