AN IMPROVED SYNTHESIS OF OLIGODEOXYRIBONUCLEOSIDE PHOSPHOROTHIOATES

寡脱氧核糖核苷硫代磷酸酯的改进合成

• 批准号: 3804710
• 负责人: S L BEAUCAGE
• 金额: --
• 依托单位国家: 美国
• 资助国家: 美国
• 起止时间: 至
• 项目状态: 未结题
• 来源: https://reporter.nih.gov/project-details/3804710
• 关键词: deoxyribonucleosides; nucleic acid chemical synthesis; nucleotide analog; thiophosphate

The process Patent pertaining to the use of 3H-1,2-benzodithiole-3-one1,1- dioxide as a sulfur-transfer reagent in the synthesis of oligodeoxyribonucleoside phosphorothioates, filed by us in late 1989, has been issued by the U.S. Patent Office in March 1991. The reagent is now commercially available albeit at an outrageous price. To facilitate the accessibility of the reagent to academic laboratories (especially oligonucleotide synthesis core facilities ) Judith B. Regan and the P>I> have scaled up the preparation of the sulfurizing reagent to ca. 125 gr by a modified procedure with respect to that published in our laboratory. This improved procedure will be submitted in Organic Syntheses by late July. The conversion of oligonucleoside phosphorothioates into oligonucleoside phosphoroamidates (another class of oligonucleotide analogues) via an oxidative aminolysis is currently being investigated in our laboratory.

与~3H-1，2-苯并二硫-3-酮-1，1-酮的用途有关的工艺专利 二氧化硫作为硫转移剂在合成中的应用 低聚脱氧核糖核苷硫代磷酸，由我们在1989年底提交，具有 由美国专利局于1991年3月发布。试剂现在是 商业上可以买到，尽管价格高得离谱。 以方便学术实验室获取试剂 (特别是寡核苷酸合成核心设施)朱迪思·B·里根和 P&gt；I&gt；已经扩大了硫化试剂的制备规模，使其成为一种新型的硫化剂。 125GR通过与我们在我们的 实验室。这一改进的程序将在有机合成中提交 到七月下旬。 硫代低聚核苷转化为低聚核苷 亚磷酰胺(另一类寡核苷酸类似物)通过一个 氧化氨解反应目前正在我们实验室进行研究。