一种2’-脱氧尿嘧啶核苷的合成方法研究  

Study on a Synthetic Method of 2’-Deoxyuridine

作　　者：李涛 Li Tao

机构地区：[1]新乡拓新药业股份有限公司,河南新乡453000

出　　处：《化工设计通讯》2021年第9期198-199,共2页Chemical Engineering Design Communications

摘　　要：以较为廉价易得的2,2’-O-环尿苷出发,经质子酸催化和碘化钠反应得到2’-脱氧-2’-碘-尿嘧啶核苷,然后经过钯碳加氢脱碘,以两步总收率83.7%的收率得到2’-脱氧尿苷,2,2’-O-环尿苷开环反应条件经过优化采用了对甲基苯磺酸为催化剂的最优条件,以91%的收率得到2’-碘-2’-脱氧核苷,该方法原料廉价易得,反应步骤短,解决了传统方法中气味大、原料价格高的问题,具有一定的应用前景。Starting from the cheaper and easily available 2,2’-O-cyclic uridine,2’-deoxy-2’-iodo-uridine is obtained by the reaction of proton acid catalyzed by sodium iodide,and then added with palladium on carbon.Hydrodeiodination,2’-deoxyuridine was obtained with a total yield of 83.7% in two steps.The 2,2’-O-cyclic uridine ring-opening reaction conditions were optimized and p-toluenesulfonic acid was used as the catalyst.Under the optimal conditions,2’-iodo-2’-deoxynucleoside was obtained with a yield of 91%.The method has low-cost and easy-to-obtain raw materials and short reaction steps.It solves the problems of large odor and high raw material price in traditional methods,and has certain advantages.Application prospects.

关 键 词：2 2’-O-环尿苷 质子酸 钯碳加氢 

分 类 号：TQ463[化学工程—制药化工]