Department of Medical Genome Sciences, Graduate School of Frontier Sciences, The University of Tokyo , Bioscience Building 702, 5-1-5 Kashiwanoha, Kashiwa, Chiba 277-8562, Japan .
J Org Chem. 2014 Apr 18;79(8):3465-72. doi: 10.1021/jo500185b. Epub 2014 Mar 28.
Recently, P-boronated oligonucleotides have been attracting much attention as potential therapeutic oligonucleotides. In this study, we developed H-boranophosphonate oligonucleotide bearing a borano group and hydrogen atom on the internucleotidic phosphorus and demonstrated that this novel P-boronated oligonucleotide is a versatile precursor to various P-boronated oligonucleotides such as boranophosphate, boranophosphorothioate, and boranophosphoramidate. The method was also applicable to the synthesis of a locked nucleic acid-modified boranophosphate oligonucleotide, which exhibited a dramatically enhanced affinity to complementary oligonucleotides.
最近，带有硼原子的寡核苷酸作为有潜力的治疗性寡核苷酸引起了广泛关注。在这项研究中，我们开发了一种带有硼烷基团和氢原子的 H-硼膦酸寡核苷酸，并证明这种新型的 P-硼化寡核苷酸是各种 P-硼化寡核苷酸（如硼代磷酸酯、硼代硫代磷酸酯和硼代磷酰胺酯）的多功能前体。该方法也适用于合成修饰后的锁核酸硼代磷酸酯寡核苷酸，其对互补寡核苷酸的亲和力显著增强。
