1048955-49-2Relevant academic research and scientific papers
Synthesis of 8-substituted xanthines via 5,6-diaminouracils: an efficient route to A2A adenosine receptor antagonists
Dong, Ma,Sitkovsky, Mikhail,Kallmerten, Amy E.,Jones, Graham B.
, p. 4633 - 4635 (2008)
A one-pot route to 8-substituted xanthines has been developed from 5,6-diaminouracils and carboxaldehydes. The process, promoted by (bromodimethyl)sulfonium bromide, is mild and efficient and eliminates the need for external oxidants. Yields are good and the process is applicable to a range of substrates including a family of A2A adenosine receptor antagonists. Preparation of a new analog of the antagonist KW-6002 is presented, and in situ bromination of aryl substituted products demonstrated.
An efficient route to xanthine based A2A adenosine receptor antagonists and functional derivatives
Labeaume, Paul,Dong, Ma,Sitkovsky, Michail,Jones, Elizabeth V.,Thomas, Rhiannon,Sadler, Sara,Kallmerten, Amy E.,Jones, Graham B.
supporting information; experimental part, p. 4155 - 4157 (2010/10/21)
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 A2A 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.
