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

Org Biomol Chem. 2010 Sep 21;8(18):4155-7. doi: 10.1039/c003382k. Epub 2010 Jul 23.

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.

MeSH terms

  • 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

Substances

  • Adenosine A2 Receptor Antagonists
  • Prodrugs
  • Purines
  • Receptor, Adenosine A2A
  • Xanthine
  • istradefylline