Efficient and Facile Synthesis of Acrylamide Libraries for Protein-Guided Tethering

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• 作者：Charlotte E. Allen ; Peter R. Curran ; Andrew S. Brearley ; Valerie Boissel ; Lilya Sviridenko ; Neil J. Press ; Jeffrey P. Stonehouse ; Alan Armstrong
• 刊名：Organic Letters
• 出版年：2015
• 出版时间：February 6, 2015
• 年：2015
• 卷：17
• 期：3
• 页码：458-460
• 全文大小：209K
• ISSN：1523-7052

文摘

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, an efficient and facile method is reported for the preparation of acrylamide libraries from a diverse range of amine fragments using a solid-supported quaternary amine base.