Investigation of a Facile Synthetic Method for Phosphorothioate Dimer Synthons In Oligonucleotide Phosphorothioates Synthesis |
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| Authors: | Takanori Miyashita Kohei Yamada Kazuhiko Kondo Kenya Mori Kazuo Shinozuka |
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| Affiliation: | 1. Department of Chemistry, Faculty of Engineering , Gunma University , Kiryu, 376-8515, Japan;2. Chemistry Lab., Yamasa Corporation , 2-10-1 Araoicho, Choshi, Chiba, 288-0056, Japan |
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| Abstract: | Abstract A facile synthetic method of a phosphorothioate dimer block was investigated. Dinucleoside phosphite triester intermediates were obtained in one-pot synthesis by the coupling of a protected nucleoside bearing free 5′-OH and a protected nucleoside bearing free 3′-OH in the presence of phosphorous trichloride (PCl3) and 1,2,4-triazole. The intermediates were easily sulfurized to afford the desired phosphorothioate dimer blocks in 33-64% overall yields. |
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