N-15 Double-Labeled Guanosine from Inosine through Ring-Opening-Ring-Closing and One-Pot Pd-Catalyzed C-O and C-N Cross-Coupling Reactions

[摘要]：[N,1-N-15(2)]-Guanosine, or [1,NH2-N-15(2)]-guanosine, and derivatives were prepared from tri-O-acetylinosine, via N-nitration and reaction with (NH2OH)-N-15, followed by conversion of the N-15-labeled 1-hydroxyinosine to the corresponding 2,6-dichloropurine riboside. The sequential one-pot C-O and C-N key couplings of this dichloro derivative with PhCH2OH and (PhCONH2)-N-15 or (PrCONH2)-Pr-i-N-15 was achieved in good overall yields, with Pd(0)-Xantphos as the best choice of five different catalytic systems examined.

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