Stonehouse, Jeffrey, Press, Neil, Boissel, Valerie, Curran, Peter, Sviridenko, Lilya, Allen, Charlotte, 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