AN IMPROVED SYNTHESIS OF OLIGODEOXYRIBONUCLEOSIDE PHOSPHOROTHIOATES

与使用3H-1,2-苯并二硫醇-3-one1,1-相关的方法专利 二氧化硫在合成中作为硫转移试剂 寡脱氧核糖核苷硫代磷酸酯，由我们于 1989 年底提交， 1991年3月由美国专利局颁发。该试剂现为 尽管价格昂贵，但可以在市场上买到。 促进学术实验室获取试剂 （特别是寡核苷酸合成核心设施）Judith B. Regan 和 P>I>已将硫化剂的制备规模扩大到约。 125 gr 通过修改程序相对于我们发布的 实验室。 这一改进的程序将在《有机合成》中提交 到七月下旬。 寡核苷硫代磷酸酯转化为寡核苷 氨基磷酸酯（另一类寡核苷酸类似物）通过 我们的实验室目前正在研究氧化氨解作用。

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.