AN IMPROVED SYNTHESIS OF OLIGODEOXYRIBONUCLEOSIDE PHOSPHOROTHIOATES

关于3 H-1，2-苯并二硫杂环戊烯-3-酮1，1- 二氧化物作为硫转移试剂在合成 我们于1989年底提交了寡脱氧核苷硫代磷酸， 美国专利局于1991年3月发布。 试剂现在 尽管价格高得离谱，但市场上还是可以买到的。 方便学术实验室使用试剂 （特别是寡核苷酸合成核心设施）朱迪思B。里根和 P>I>已经将硫化剂的制备放大到约100%。 125 gr，根据我们的 实验室 这一改进的程序将在《有机合成》杂志上发表 到七月下旬。 硫代磷酸酯转化为糖苷 氨基磷酸酯（另一类寡核苷酸类似物）通过 氧化氨解目前正在我们实验室进行研究。

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.