Synthesis of 6- and 8-alkynylated purines and their ribonucleosides by the coupling of halopurines with alkynes.


Coupling reaction of 6-iodo- or 6-chloropurine with alkynes in the presence of (PPh3) 2PdCl2-CuI catalyst in triethylamine to give 6-alkynylated purines was achieved by the use of dipolar aprotic solvent as co-solvent. Under the reaction conditions, ribonucleoside as well as its tri-O-acetate of 6-chloropurine also gave the corresponding alkynylated… (More)


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