It is provided an achiral, non-nucleosidic backbone for phosphoramidites that can be inserted with high yields in nucleic acid strands and sequence-controlled oligo(phosphodiester)s through solid phase synthesis (SPS) using a DNA synthesizer. From this backbone, platforms with useful chemical handles were synthesized, further functionalized, transformed into phosphoramidites and attached to nucleic acid strands and sequence-controlled oligo(phosphodiester)s. The backbone is based on a tertiary amine with a 3-6 carbon spacer between the central nitrogen and the two external hydroxyls. The spacer has been optimized to increase coupling yields and stability.
提供了一种不对映体、非核苷酸骨架的
磷酰胺酯,可以通过固相合成(
SPS)在核酸链和序列控制的寡聚(
磷酸二酯)中高产率地插入,并使用DNA合成器。从这种骨架中,合成了具有有用
化学手柄的平台,进一步功能化,转化为
磷酰胺酯,并连接到核酸链和序列控制的寡聚(
磷酸二酯)。该骨架基于具有中心氮和两个外部羟基之间的3-6碳间隔的三级胺。已经优化了间隔以提高偶联产率和稳定性。