An efficient solid-phase synthesis of 3-carboxycoumarins based on a scaffold-polymer-bound cyclic malonic ester

2003 ◽  
Vol 2003 (6) ◽  
pp. 354-355 ◽  
Author(s):  
Jing Tang ◽  
Xian Huang
Keyword(s):  
Solid Phase Synthesis ◽  
Solid Phase ◽  
Malonic Ester ◽  
Phase Synthesis

Novel and Efficient Solid-Phase Synthesis of 4,6-Disubstituted 4,5-Dihydro-3(2H)-Pyridazinones

2003 ◽  
Vol 2003 (9) ◽  
pp. 599-600
Author(s):  
Jing Tang ◽  
Xian Huang
Keyword(s):  
High Purity ◽  
Good Yield ◽  
Solid Phase Synthesis ◽  
Solid Phase ◽  
Malonic Ester ◽  
Polymeric Support ◽  
Subsequent Reaction ◽  
Phase Synthesis

The resin-bound 5-monosubstituted cyclic malonic ester 3 was generated and reacted with an α–bromoketone to give the corresponding 5,5-disubstituted cyclic malonic ester resin (4). Subsequent reaction with hydrazine resulted in cyclisation with concomitant cleavage from the polymeric support to release the final products, 4,6-disubstituted 4,5-dihydro-3(2 H)-pyridazinones, in good yield and high purity.

Synthesis and Screening of A DNA-Encoded Library of Non-Peptidic Macrocycles

2020 ◽  
Author(s):  
Eric Koesema ◽  
Animesh Roy ◽  
Nicholas G. Paciaroni ◽  
Thomas Kodadek
Keyword(s):  
Solid Phase Synthesis ◽  
Solid Phase ◽  
Cell Permeability ◽  
Phase Synthesis ◽  
Protein Ligands ◽  
High Affinity ◽  
Scaffold Diversity

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.

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