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Efficient and facile synthesis of acrylamide libraries for protein-guided tethering

Stonehouse, Jeffrey and Press, Neil and Boissel, Valerie and Curran, Peter and Sviridenko, Lilya and Allen, Charlotte and Brearley, Andrew and Armstrong, Alan (2015) Efficient and facile synthesis of acrylamide libraries for protein-guided tethering. Organic Letters.

Abstract

A kinetic template-guided tethering (KTGT) strategy has been developed for the site-directed discovery of fragments that bind to defined protein surfaces, where acrylamide-modified fragments can be irreversibly captured in a protein templated, conjugate addition reaction. Herein, we report an efficient and facile method for the preparation of acrylamide libraries from a diverse range of amine fragments, using a solid-supported quaternary amine base.

Item Type: Article
Date Deposited: 02 May 2016 23:45
Last Modified: 02 May 2016 23:45
URI: https://oak.novartis.com/id/eprint/22861

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