Heterogeneous Diazo-Transfer Reaction:  A Facile Unmasking of Azide Groups on Amine-Functionalized Insoluble Supports for Solid-Phase Synthesis

2006 ◽  
Vol 71 (26) ◽  
pp. 9791-9796 ◽  
Author(s):  
A. K. Oyelere ◽  
P. C. Chen ◽  
L. P. Yao ◽  
N. Boguslavsky
2009 ◽  
Vol 74 (24) ◽  
pp. 9280-9286 ◽  
Author(s):  
S. Sibel Erdem ◽  
Irina V. Nesterova ◽  
Steven A. Soper ◽  
Robert P. Hammer

2020 ◽  
Author(s):  
Eric Koesema ◽  
Animesh Roy ◽  
Nicholas G. Paciaroni ◽  
Thomas Kodadek

There is considerable interest in the development of libraries of non-peptidic macrocycles as a source of ligands for difficult targets. We report here the solid-phase synthesis of a DNA-encoded library of several hundred thousand thioether-linked macrocycles. The library was designed to be highly diverse with respect to backbone scaffold diversity and to minimize the number of amide N-H bonds, which compromise cell permeability. The utility of the library as a source of protein ligands is demonstrated through the isolation of compounds that bind streptavidin, a model target, with high affinity.


Sign in / Sign up

Export Citation Format

Share Document