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Organic & biomolecular chemistry

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


PMID 20652178

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.

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