Palladium-Catalyzed Animation of 6-Chloropurine. Synthesis of N⁶-Substituted Adenosine Analogues

Abstract

Abstract Room-temperature treatment of persilylated 6-chloro-9-β-D-ribofuranosyl-purine with a variety of aliphatic and aromatic amines, in the presence of Pd2(dba)3, BINAP and base, leads to N6-substituted adenosine analogues in fair to good yields. Coupling of chloropurine with a chiral aziridinyl diester is applied in the synthesis of a potential adenylosuccinate lyase inhibitor.