Xanthines represent a new, versatile scaffold for combinatorial chemis
try. A five-step solid-phase synthesis of xanthine derivatives is desc
ribed which includes alkylations, a nucleophilic displacement reaction
at a heterocycle and a ring closure reaction by condensation of a nit
roso function with an activated methylene group. The selected reaction
sequence allows the production of a highly diverse small-molecule com
binatorial compound library.