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A practical and scalable system for heteroaryl amino acid synthesis†
R. A. Aycock,D. B. Vogt,N. T. Jui
Chemical Science Pub Date : 10/02/2017 00:00:00 , 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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