Chimeric RNA Oligonucleotides with Triazole and Phosphate Linkages: Synthesis and RNA Interference.

Tomoko Fujino, Kanako Kogashi, Koudai Okada, Martin Mattarella, Takeru Suzuki, Kenichi Yasumoto, Kazuhiro Sogawa, Hiroyuki Isobe

Index: Chem. Asian J. 10 , 2683-8, (2016)

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Abstract

Chimeric RNA oligonucleotides with an artificial triazole linker were synthesized using solution-phase click chemistry and solid-phase automated synthesis. Scalable synthesis methods for jointing units for the chimeric structure have been developed, and after click-coupling of the jointing units with triazole linkers, a series of chimeric oligonucleotides was prepared by utilizing the well-established phosphoramidite method for the elongation. The series of chimeric 21-mer oligonucleotides that possessed the triazole linker at different strands and positions allowed for a screening study of the RNA interference to clarify the preference of the triazole modifications in small-interfering RNA molecules. © 2015 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.