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

作者:LaBeaume Paul; Dong Ma; Sitkovsky Michail; Jones Elizabeth V; Thomas Rhiannon; Sadler Sara; Kallmerten Amy E; Jones Graham B*
来源:Organic and Biomolecular Chemistry, 2010, 8(18): 4155-4157.
DOI:10.1039/c003382k

摘要

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.