Graduate School of Science, Nagoya University, Japan.
CREST, Japan Science and Technology Agency, Japan.
Org Biomol Chem. 2023 May 17;21(19):3997-4001. doi: 10.1039/d2ob02260e.
We herein report a new synthetic method for nucleoside oligophosphates based on electrophilic activation of 5'-phosphorothioate nucleotides. The treatment of phosphorothioate with 2,4-dinitrochlorobenzene (DNCB) efficiently afforded the key activated species, electrophilic thioester nucleotides (EPT-Ns), which were coupled with various phosphate reagents to afford the target nucleoside oligophosphates, including an mRNA cap analog.
我们在此报告了一种基于 5'-硫代磷酸核苷酸的亲电活化的寡核苷酸合成新方法。用 2,4-二硝基氯苯（DNCB）处理硫代磷酸酯可有效地得到关键的活化物质，亲电硫酯核苷酸（EPT-Ns），它与各种磷酸试剂偶联得到目标核苷寡磷酸酯，包括一种 mRNA 帽类似物。
