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We have previously described that the oligonucleotides containing phenylsulfide derivatives of 2-amino-6-vinylpurine nucleoside analog are activated within duplex to form cross-link toward cytidine selectively at the target site. However, the cross-linking reaction via the in-situ activation needs acidic conditions. In this paper, we wish to report that the new 2-amino-6-vinylpurine derivatives designed to have a structure of "double-activation" for in-situ activation exhibit fast cross-linking with cytidine under neutral conditions.

Efficient cross-linking reactions by functional nucleobases capable of in situ activation under neutral conditions