Issue 12, 2016

An atom-efficient and convergent approach to the preparation of NS5A inhibitors by C–H activation

Abstract

A novel approach of the convergent functionalisation of aryl dibromides to form NS5A type inhibitors using C–H activation is reported. The focus of investigation was to reduce the formation of homodimeric side product, as well as to investigate the scope of different aryl dibromides that were tolerated under the reaction conditions. The C–H activation methodology was found to give a viable synthetic route to NS5A inhibitors, with late stage functionalisation of the core portion of the molecule, albeit with some chemical functionalities not tolerated.

Graphical abstract: An atom-efficient and convergent approach to the preparation of NS5A inhibitors by C–H activation

Supplementary files

Article information

Article type
Paper
Submitted
12 Feb 2016
Accepted
25 Feb 2016
First published
25 Feb 2016
This article is Open Access
Creative Commons BY license

Org. Biomol. Chem., 2016,14, 3307-3313

An atom-efficient and convergent approach to the preparation of NS5A inhibitors by C–H activation

T. O. Moore, M. Paradowski and S. E. Ward, Org. Biomol. Chem., 2016, 14, 3307 DOI: 10.1039/C6OB00340K

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