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5′- 18O  labeled RNA oligos are important probes to investigate the mechanism of 2′- O -transphosphorylation reactions. Here we describe a general and efficient synthetic approach to the phosphoramidite derivatives of 5′- 18O  labeled nucleosides starting from the corresponding commercially available 5′- O -DMT protected nucleosides. Using this method, we prepared 5′- 18O -guanosine phosphoramidite in 8 steps (13.2% overall yield), 5′- 18O- adenosine phosphoramidite in 9 steps (10.1% overall yield) and 5′- 18O -2′-deoxyguanosine phosphoramidite in 6 steps (12.8% overall yield). These 5′- 18O  labeled phosphoramidites can be incorporated into RNA oligos by solid phase synthesis for determination of heavy atom isotope effects in RNA 2′- O -transphosphorylation reactions.

A general and efficient approach to synthesize the phosphoramidites of 5′- 18 O labeled purine nucleosides