A. Gopalsamy et H. Yang, Combinatorial synthesis of heterocycles: Solid-phase synthesis of 6-amino-2,4-dioxo-3,4-dihydro-1,3,5-triazine derivatives, J COMB CHEM, 3(3), 2001, pp. 278-283
A new solid-phase synthesis of trisubstituted 6-amino-2,4-dioxo-3,4-dihydro
-1,3,5-triazines From a resin-bound amine component is described. The amine
was readily converted to the corresponding palymerbound S-methylthiopseudo
urea, which upon reaction with secondary amines gave the disubstituted guan
idines. Cyclization of the polymer-bound guanidines with chlorocarbonylisoc
yanate afforded the triazinediones. The third point of diversity was introd
uced by the Mitsunobu reaction. The method is amenable for iterative combin
atorial library generation.