Exogenous Directing Group Free, Ligand-Enabled gamma-C(sp3)–H Arylation of Free Primary Aliphatic Amines and α-Amino Esters

10 December 2019, Version 1
This content is a preprint and has not undergone peer review at the time of posting.

Abstract

A Pdᴵᴵ-catalyzed, ligand-enabled gamma-C(sp3)–H arylation of free primary aliphatic amines and amino esters without using an exogenous directing group is reported. This reaction is compatible with unhindered free aliphatic amines, and it is also be applicable to the rapid synthesis of biologically and synthetically valuable unnatural α-amino acids. Large scale synthesis is also feasible using this method.

Keywords

C–H activation
free aliphatic amine
exogenous directing group
arylation
amino acid
ligand enabled

Supplementary materials

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Description
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Title
SILigand-NH2-Arylation-LiG-Rxiv
Description
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