scholarly journals The Synthesis of Two Combinatorial Libraries Using a 4-(2-Thienyl)-pyrrole Template

2002 ◽  
Vol 55 (12) ◽  
pp. 789 ◽  
Author(s):  
Rohan A. Davis ◽  
Anthony R. Carroll ◽  
Ronald J. Quinn
Keyword(s):  
Reductive Amination ◽  
Combinatorial Libraries ◽  
Solution Phase ◽  
Primary Amines ◽  
The Novel ◽  
Compound Library ◽  
Phase Synthesis ◽  
Parallel Solution ◽  
Tert Butyl ◽  
Solution Phase Synthesis

The synthesis of the novel biaryl compound, 4-(2-thienyl)-1H-pyrrole-2-carbaldehyde (1), by Suzuki–Miyaura coupling conditions is reported. Compound (1) was subsequently used as a combinatorial template in the parallel solution-phase synthesis of an amine and imine compound library. The amine library was produced using reductive amination conditions, and purification was achieved by a liquid–liquid partition followed by silica chromatography to afford ten amine analogues. The imine library consisted of five compounds, which were synthesized using volatile primary amines that allowed purification by evaporation. The synthesis of the novel and related biaryl carbaldehyde, tert-butyl-2-(5-formyl-1H-pyrrol-3-yl)-1H-pyrrole-1-carboxylate (2) is also reported.

Parallel Solution-phase Synthesis of (2S,4E)-4-(Arylaminomethylidene)pyroglutamic Acids

2010 ◽  
Vol 65 (7) ◽  
pp. 811-820 ◽  
Author(s):  
Jurij Svete ◽  
Uroš Grošelj ◽  
Jernej Baškovč ◽  
Georg Dahmann ◽  
Branko Stanovnik
Keyword(s):  
Double Bond ◽  
Nmr Spectroscopy ◽  
Carboxylic Acids ◽  
Solution Phase ◽  
Phase Synthesis ◽  
Parallel Solution ◽  
Tert Butyl ◽  
Solution Phase Synthesis

A library of twelve N(4´)-substituted di-tert-butyl (2S,4E)-4-arylaminomethylidene-5-oxopyrrolidine-1,2-dicarboxylates 6/6´a - l were prepared in 47 - 90% yield by parallel acid-catalysed treatment of di-tert-butyl (2S,4E)-4-[(dimethylamino)methylidene]-5-oxopyrrolidine-1,2-dicarboxylate (4) with anilines 5a - j, ethyl glycinate (5k), and ethyl β -alaninate (3l). Acidolytic deprotection of compounds 6a - c, e - j afforded the corresponding (2S,4E)-4-arylaminomethylidene-5-oxopyrrolidine-2-carboxylic acids 7a - c, e - j in 39 - 99% yield. The configuration around the C=C double bond in the enaminones 6 and 7 was determined by NMR spectroscopy.

Polymer-Assisted Parallel Solution Phase Synthesis of Substituted Benzimidazoles.

ChemInform ◽  
2010 ◽  
Vol 33 (35) ◽  
pp. 123-123
Author(s):  
Young K. Yun ◽  
John A. Porco Jr. ◽  
Jeff Labadie
Keyword(s):  
Solution Phase ◽  
Phase Synthesis ◽  
Parallel Solution ◽  
Solution Phase Synthesis

ChemInform Abstract: One-Pot Parallel Solution-Phase Synthesis of 1-Substituted 4-(2-Aminoethyl)-1H-pyrazol-5-ols.

ChemInform ◽  
2009 ◽  
Vol 40 (4) ◽  
Author(s):  
David Kralj ◽  
Ana Novak ◽  
Georg Dahmann ◽  
Uros Groselj ◽  
Anton Meden ◽  
...  
Keyword(s):  
Solution Phase ◽  
One Pot ◽  
Phase Synthesis ◽  
Parallel Solution ◽  
Solution Phase Synthesis

Bis-enaminone Based Parallel Solution-Phase Synthesis of 1,4-Dihydropyridine Derivatives

2009 ◽  
Vol 11 (3) ◽  
pp. 500-507 ◽  
Author(s):  
Jernej Baškovč ◽  
David Bevk ◽  
Branko Stanovnik ◽  
Jurij Svete
Keyword(s):  
Solution Phase ◽  
Phase Synthesis ◽  
Parallel Solution ◽  
Solution Phase Synthesis ◽  
Dihydropyridine Derivatives

Parallel Solution-Phase Synthesis

ChemInform ◽  
2007 ◽  
Vol 38 (29) ◽  
Author(s):  
Norton P. Peet ◽  
Hwa-Ok Kim
Keyword(s):  
Solution Phase ◽  
Phase Synthesis ◽  
Parallel Solution ◽  
Solution Phase Synthesis

scholarly journals Macrocycle synthesis strategy based on step-wise “adding and reacting” three components enables screening of large combinatorial libraries

2020 ◽  
Vol 11 (30) ◽  
pp. 7858-7863 ◽  
Author(s):  
Ganesh K. Mothukuri ◽  
Sangram S. Kale ◽  
Carl L. Stenbratt ◽  
Alessandro Zorzi ◽  
Jonathan Vesin ◽  
...  
Keyword(s):  
Chemical Reactions ◽  
Combinatorial Libraries ◽  
Solution Phase ◽  
Thrombin Inhibitor ◽  
Phase Synthesis ◽  
Synthesis Strategy ◽  
Solution Phase Synthesis ◽  
Three Components

Combination of three efficient chemical reactions allows for solution-phase synthesis of 3780 macrocycles and identification of potent thrombin inhibitor.

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