Synthesis of 8-substituted xanthines via 5,6-diaminouracils: an efficient route to A2A adenosine receptor antagonists |
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| Authors: | Ma Dong Amy E Kallmerten |
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| Institution: | a Bioorganic and Medicinal Chemistry Laboratories, Department of Chemistry and Chemical Biology, Northeastern University, Boston, MA 02115, United States
b New England Inflammation and Tissue Protection Institute, Northeastern University, Boston, MA 02115, United States |
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| Abstract: | 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. |
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| Keywords: | Xanthine (Bromodimethyl)sulfonium bromide Adenosine antagonist Diaminouracils |
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