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The Groebke‐Blackburn‐Bienaymé Reaction

Boltjes, André ; Dömling, Alexander

European journal of chemistry, 2019-11, Vol.2019 (42), p.7007-7049 [Periódico revisado por pares]

United States: Wiley Subscription Services, Inc

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  • Título:
    The Groebke‐Blackburn‐Bienaymé Reaction
  • Autor: Boltjes, André ; Dömling, Alexander
  • Assuntos: Biological activity ; Chemical space ; FDA approval ; Imidazo[1,2‐a]pyridine ; Isocyanides ; Multicomponent reactions ; Organic chemistry ; Scaffolds
  • É parte de: European journal of chemistry, 2019-11, Vol.2019 (42), p.7007-7049
  • Notas: ObjectType-Article-1
    SourceType-Scholarly Journals-1
    ObjectType-Feature-2
    content type line 23
  • Descrição: Imidazo[1,2‐a]pyridine is a well‐known scaffold in many marketed drugs, such as Zolpidem, Minodronic acid, Miroprofen and DS‐1 and it also serves as a broadly applied pharmacophore in drug discovery. The scaffold revoked a wave of interest when Groebke, Blackburn and Bienaymé reported independently a new three component reaction resulting in compounds with the imidazo[1,2‐a]‐heterocycles as a core structure. During the course of two decades the Groebke Blackburn Bienaymé (GBB‐3CR) reaction has emerged as a very important multicomponent reaction (MCR), resulting in over a hundred patents and a great number of publications in various fields of interest. Now two compounds derived from GBB‐3CR chemistry received FDA approval. To celebrate the first 20 years of GBB‐chemistry, we present an overview of the chemistry of the GBB‐3CR, including an analysis of each of the three starting material classes, solvents and catalysts. Additionally, a list of patents and their applications and a more in‐depth summary of the biological targets that were addressed, including structural biology analysis, is given. Over the past 20 years, the Groebke‐Blackburn‐Bienaymè reaction, one of the youngest IMCRs, has gained much interest. Since 1998, a total of >200 peer reviewed publications and >100 patent applications have been reported. This overview describes the development of the GBB reaction and includes a tabular analysis to show exactly which reagents were reported as one of three components in the GBB reaction.
  • Editor: United States: Wiley Subscription Services, Inc
  • Idioma: Inglês
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  • Realização: ABCD-USP USP   Logos de Redes Sociais: Freepik

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