Synthesis and biophysical characterization of R-6′-Me-α-L-LNA modified oligonucleotides
Synthesis and biophysical characterization of R-6′-Me-α-L-LNA modified oligonucleotides
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DOI：
10.1016/j.bmcl.2010.12.119
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发表时间：
2011-02-15
影响因子：
2.7
通讯作者：
Swayze, Eric E.
中科院分区：
文献类型：
--
作者：
Seth, Punit P.;Yu, Jinghua;Swayze, Eric E.
本文报道了R-6‘-Me-α-L-LNA的合成和生物物理性质，该化合物在α-L-LNA的2’，4‘-桥基上含有甲基。从一种已知的糖中间体出发，经过14步和8次层析纯化，有效地完成了尿嘧啶核酸亚磷酰胺的合成。生物物理评价表明，沿着主槽边缘的取代不会损害α-L-低聚核糖核酸修饰的寡核苷酸的高亲和力双链形成能力。(C)2010爱思唯尔有限公司。保留所有权利。
The synthesis and biophysical properties of R-6`-Me-alpha-L-LNA, which has a methyl group in the ( R) configuration on the 2`,4`-bridging substituent of alpha-L-LNA, is reported. The synthesis of the uracil nucleobase phosphoramidite was efficiently accomplished in 14 steps and 8 chromatographic purifications starting from a known sugar intermediate. Biophysical evaluation revealed that substitution along the edge of the major groove does not impair the high affinity duplex forming ability of alpha-L-LNA modified oligonucleotides. (c) 2010 Elsevier Ltd. All rights reserved.