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<i>anti</i>-Selective synthesis of β-boryl-α-amino acid derivatives by Cu-catalysed borylamination of α,β-unsaturated esters

Soshi Nishino, Yuji Nishii, Koji Hirano

2022Chemical Science26 citationsDOIOpen Access PDF

Abstract

-diastereoselectivity (up to >99 : 1), which is difficult to obtain by the established methods. A chiral phosphoramidite ligand also successfully induces the enantioselectivity, giving the optically active β-borylated α-amino acids. The products can be stereospecifically transformed into β-functionalised α-amino acids, which are of potent interest in medicinal chemistry.

Topics & Concepts

ChemistryCombinatorial chemistryAmino acidOrganic chemistryBiochemistryOrganoboron and organosilicon chemistryChemical Synthesis and AnalysisAdvanced Synthetic Organic Chemistry
<i>anti</i>-Selective synthesis of β-boryl-α-amino acid derivatives by Cu-catalysed borylamination of α,β-unsaturated esters | Litcius