A practical and scalable system for heteroaryl amino acid synthesis?

Chemical Science Pub Date: 2017-10-02 DOI: 10.1039/C7SC03612D

Abstract

A robust system for the preparation of β-heteroaryl α-amino acid derivatives has been developed using photoredox catalysis. This system operates via regiospecific activation of halogenated pyridines (or other heterocycles) and conjugate addition to dehydroalanine derivatives to deliver a wide range of unnatural amino acids. This process was conducted with good efficiency on large scale, the application of these conditions to amino ketone synthesis is shown, and a simple protocol is given for the preparation of enantioenriched amino acid synthesis, from a number of radical precursors.

Graphical abstract: A practical and scalable system for heteroaryl amino acid synthesis
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