An efficient route to xanthine based A2A adenosine receptor antagonists and functional derivatives

Paul LaBeaume; Ma Dong; Michail Sitkovsky; Elizabeth V. Jones; Rhiannon Thomas; Sara Sadler; Amy E. Kallmerten; Graham B. Jones

doi:10.1039/C003382K

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An efficient route to xanthine based A_2A adenosine receptorantagonists and functional derivatives†

Paul LaBeaume,^a Ma Dong,^a Michail Sitkovsky,^a Elizabeth V. Jones,^a Rhiannon Thomas,^a Sara Sadler,^a Amy E. Kallmerten^a and Graham B. Jones*^a

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* Corresponding authors

^a Department of Chemistry and Chemical Biology, Northeastern University, Boston, MA., USA
E-mail: gr.jones@neu.edu
Fax: (+)1 617 3738795

Abstract

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.

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Supplementary files

Experimental procedures, structural proofs, NMR of the products PDF (6529K)

Article information

DOI: https://doi.org/10.1039/C003382K
Article type: Paper
Submitted: 22 Feb 2010
Accepted: 24 Jun 2010
First published: 23 Jul 2010

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Org. Biomol. Chem., 2010,8, 4155-4157

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An efficient route to xanthine based A_2A adenosine receptor antagonists and functional derivatives

P. LaBeaume, M. Dong, M. Sitkovsky, E. V. Jones, R. Thomas, S. Sadler, A. E. Kallmerten and G. B. Jones, Org. Biomol. Chem., 2010, 8, 4155 DOI: 10.1039/C003382K

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Organic & Biomolecular Chemistry