An efficient route to xanthine based A2A adenosine receptor antagonists and functional derivatives
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.
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)
Synthesis of 8-substituted xanthines via 5,6-diaminouracils: an efficient route to A2A adenosine receptor antagonists
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.
Dong, Ma,Sitkovsky, Mikhail,Kallmerten, Amy E.,Jones, Graham B.
p. 4633 - 4635
(2008/09/21)
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