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Forming All‐Carbon Quaternary Stereocenters by Organocatalytic Aminomethylation: Concise Access to β<sup>2,2</sup>‐Amino Acids

Kai Wang, Jianliang Yu, Ying Shao, Shengbiao Tang, Jiangtao Sun

2020Angewandte Chemie International Edition42 citationsDOI

Abstract

Abstract The asymmetric synthesis of β 2,2 ‐amino acids remains a formidable challenge in organic synthesis. Here a novel organocatalytic enantioselective aminomethylation of ketenes with stable and readily available N,O‐acetals is reported, providing β 2,2 ‐amino esters bearing an all‐carbon quaternary stereogenic center in high enantiomeric ratios with a catalytic amount of chiral phosphoric acid. Typically, this transformation probably proceeds through an asymmetric counter‐anion‐directed catalysis. As a result, a concise, practical, and atom‐economic protocol toward rapidly access to β 2,2 ‐amino acids has been developed.

Topics & Concepts

StereocenterEnantioselective synthesisOrganocatalysisChemistryCatalysisAmino acidEnantiomerPhosphoric acidCarbon fibersAsymmetric carbonCombinatorial chemistryQuaternary carbonBrønsted–Lowry acid–base theoryCarbon atomOrganic chemistryStereochemistryOptically activeRing (chemistry)Materials scienceComposite materialComposite numberBiochemistryChemical Synthesis and AnalysisAsymmetric Hydrogenation and CatalysisAsymmetric Synthesis and Catalysis
Forming All‐Carbon Quaternary Stereocenters by Organocatalytic Aminomethylation: Concise Access to β<sup>2,2</sup>‐Amino Acids | Litcius