A highly efficient solid-phase synthesis of 1,3-substituted xanthines.
A first solid-phase route to 1,3-substituted xanthines has been developed using PS-MB-CHO resin. Cyclocondensation of the polymer-bound aminoimidazole with isocyanates followed by alkylation provided 1,3-substituted xanthines in high yields. Libraries of 12 xanthines and 4 thioxanthines were prepared.
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