title: An efficient route to xanthine based A(2A) adenosine receptor antagonists and functional derivatives.
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.
authors.affiliation: Department of Chemistry and Chemical Biology, Northeastern University, Boston, MA 02115, USA.
authors.forename: Paul
authors.initials: P
authors.lastname: Labeaume
authors.forename: Ma
authors.initials: M
authors.lastname: Dong
authors.forename: Michail
authors.initials: M
authors.lastname: Sitkovsky
authors.forename: Elizabeth V
authors.initials: EV
authors.lastname: Jones
authors.forename: Rhiannon
authors.initials: R
authors.lastname: Thomas
authors.forename: Sara
authors.initials: S
authors.lastname: Sadler
authors.forename: Amy E
authors.initials: AE
authors.lastname: Kallmerten
authors.forename: Graham B
authors.initials: GB
authors.lastname: Jones
mesh_terms: D058917:Adenosine A2 Receptor Antagonists / Q000138:chemical synthesis* / Q000737:chemistry; D015394:Molecular Structure; D011355:Prodrugs / Q000138:chemical synthesis* / Q000737:chemistry; D011687:Purines / Q000138:chemical synthesis* / Q000737:chemistry; D043705:Receptor, Adenosine A2A / Q000378:metabolism; D013237:Stereoisomerism; D019820:Xanthine / Q000138:chemical synthesis* / Q000737:chemistry
chemical_list: D058917:Adenosine A2 Receptor Antagonists; D011355:Prodrugs; D011687:Purines; D043705:Receptor, Adenosine A2A; D019820:Xanthine; C111599:istradefylline