- An efficient route to xanthine based A(2A) adenosine receptor antagonists and functional derivatives.
An efficient route to xanthine based A(2A) adenosine receptor antagonists and functional derivatives.
Organic & biomolecular chemistry (2010-07-24)
Paul Labeaume, Ma Dong, Michail Sitkovsky, Elizabeth V Jones, Rhiannon Thomas, Sara Sadler, Amy E Kallmerten, Graham B Jones
PMID20652178
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.
MATERIALS