An efficient route to xanthine based A(2A) adenosine receptor antagonists and functional derivatives

A one-pot route to 8-substituted xanthines has been developed from 5,6-diaminouracils and carboxaldehydes. Yields are good and the process applicable to a range of substrates including a family of A(2A) adenosine receptor antagonists. A new route to the KW-6002 family of antagonists is presented inc...

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Veröffentlicht in:	Organic & biomolecular chemistry 2010-09, Vol.8 (18), p.4155-4157
Hauptverfasser:	Labeaume, Paul, Dong, Ma, Sitkovsky, Michail, Jones, Elizabeth V, Thomas, Rhiannon, Sadler, Sara, Kallmerten, Amy E, Jones, Graham B
Format:	Artikel
Sprache:	eng
Schlagworte:	Adenosine A2 Receptor Antagonists - chemical synthesis Adenosine A2 Receptor Antagonists - chemistry Molecular Structure Prodrugs - chemical synthesis Prodrugs - chemistry Purines - chemical synthesis Purines - chemistry Receptor, Adenosine A2A - metabolism Stereoisomerism Xanthine - chemical synthesis Xanthine - chemistry
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Zusammenfassung:	A one-pot route to 8-substituted xanthines has been developed from 5,6-diaminouracils and carboxaldehydes. Yields are good and the process applicable to a range of substrates including a family of A(2A) adenosine receptor antagonists. A new route to the KW-6002 family of antagonists is presented including a pro-drug variant, and application to related image contrast agents developed.
ISSN:	1477-0539
DOI:	10.1039/c003382k