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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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Supplementary files

Article information


Submitted
25 Jan 2011
Accepted
10 Mar 2011
First published
10 Mar 2011

Org. Biomol. Chem., 2011,9, 4144-4149
Article type
Paper

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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