Synthesis of thiazolo[4,5-]pyrimidine derivatives based on purine solid-phase synthesis.

Solid-phase synthesis was employed to construct a library of thiazolo[4,5-]pyrimidine derivatives. The free amide at the 5-position of the thiazole, which was previously difficult to introduce the Thorpe-Ziegler reaction, was successfully optimized in solid-phase synthesis using a 2,4-dimethoxy-substituted scaffold, and using iodine as a catalyst, the reaction with aldehyde successfully synthesized thiazolo-pyrimidinone derivatives. To synthesize thiazolo[4,5-]pyrimidine derivatives, the direct amination reaction using BOP was successfully optimized.