The Gewald multicomponent reaction.
The Gewald reaction of sulfur, cyanoacetic acid derivatives, and oxo-component (G-3CR) yielding highly substituted 2-aminothiophene derivatives has seen diverse applications in combinatorial and medicinal chemistry. Its products are of great use in pharmaceutical industry mainly as small molecular weight inhibitors. We herein review synthetic scope and variations, usage, and structural biology of Gewald products.
Huang
Yijun
Y
Department of Pharmaceutical Sciences and Chemistry, University of Pittsburgh, Pittsburgh, PA 15261, USA.
Dömling
Alexander
A
D000085:Acetates / Q000737:chemistry*; D000595:Amino Acid Sequence; D000818:Animals; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D013455:Sulfur / Q000737:chemistry*; D013876:Thiophenes / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology
D000085:Acetates; D004791:Enzyme Inhibitors; D013876:Thiophenes; D013455:Sulfur; C007170:cyanoacetic acid