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Issue 11, 2011
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Groebke multicomponent reaction and subsequent nucleophilic aromatic substitution for a convenient synthesis of 3,8-diaminoimidazo[1,2-a]pyrazines as potential kinase inhibitors

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Abstract

In a program aimed at discovering novel protein kinase inhibitors, a convenient synthesis of 3,8-diaminoimidazo[1,2-a]pyrazines has been developed exploiting the isocyanide-based multicomponent Blackburn reaction, followed by a nucleophilic aromatic substitution with ammonia or primary and secondary amines. The potential of the reported scaffold is strengthened by the inhibition of STAT5-dependent transcription displayed by four of the synthesized compounds.

Graphical abstract: Groebke multicomponent reaction and subsequent nucleophilic aromatic substitution for a convenient synthesis of 3,8-diaminoimidazo[1,2-a]pyrazines as potential kinase inhibitors

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Publication details

The article was received on 25 Jan 2011, accepted on 10 Mar 2011 and first published on 10 Mar 2011


Article type: Paper
DOI: 10.1039/C1OB05336A
Citation: Org. Biomol. Chem., 2011,9, 4144-4149
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    Groebke multicomponent reaction and subsequent nucleophilic aromatic substitution for a convenient synthesis of 3,8-diaminoimidazo[1,2-a]pyrazines as potential kinase inhibitors

    M. Guasconi, X. Lu, A. Massarotti, A. Caldarelli, E. Ciraolo, G. C. Tron, E. Hirsch, G. Sorba and T. Pirali, Org. Biomol. Chem., 2011, 9, 4144
    DOI: 10.1039/C1OB05336A

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