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

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 fac...

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Bibliographic Details
Published in:Organic letters 2015-02, Vol.17 (3), p.458-460
Main Authors: Allen, Charlotte E, Curran, Peter R, Brearley, Andrew S, Boissel, Valerie, Sviridenko, Lilya, Press, Neil J, Stonehouse, Jeffrey P, Armstrong, Alan
Format: Article
Language:English
Subjects:
Acrylamide - chemical synthesis
Acrylamide - chemistry
Amines - chemistry
Catalysis
Combinatorial Chemistry Techniques
Molecular Structure
Quinolines - chemical synthesis
Quinolines - chemistry
Quinolines - pharmacology
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Summary: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.
ISSN:1523-7060
1523-7052
DOI:10.1021/ol503486t