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1,2,3-O-三乙酰基-5-脱氧核糖的合成工艺研究
引用本文:朱仁发,何勇,陈仕云,邵国泉.1,2,3-O-三乙酰基-5-脱氧核糖的合成工艺研究[J].安徽医药,2008,12(1):11-12.
作者姓名:朱仁发  何勇  陈仕云  邵国泉
作者单位:1. 合肥学院化学与材料工程系,安徽,合肥,230022
2. 合肥辉佳化工科技有限公司,安徽,合肥,230051
摘    要:目的抗肿瘤药物中间体1,2,3-O-三乙酰基-5-脱氧核糖的合成。方法以肌苷为起始原料经碘化得5'-碘代-6-羟基-9-β-D-嘌呤核苷,产物氢化得产物5'-脱氧-6-羟基-9-β-D-嘌呤核苷,然后经酰化共3步反应合成1,2,3-O-三乙酰基-5-脱氧核糖。结果以肌苷为起始原料经3步反应合成了1,2,3-O-三乙酰基-5-脱氧核糖。结论本合成方法原料价廉易得,工艺简便,条件温和,总收率为38.0%,适合于工业制备。

关 键 词:1  2  3-O-三乙酰基-5-脱氧核糖  卡培他滨  化学合成  抗肿瘤
收稿时间:2007-09-17
修稿时间:2007年9月17日

Research of synthesis of 1,2,3-O-triacetyl-5-deoxy-D-riboturanose
ZHU Ren-fa,HE Yong,CHEN Shi-yun,SHAO Guo-quan.Research of synthesis of 1,2,3-O-triacetyl-5-deoxy-D-riboturanose[J].Anhui Medical and Pharmaceutical Journal,2008,12(1):11-12.
Authors:ZHU Ren-fa  HE Yong  CHEN Shi-yun  SHAO Guo-quan
Institution:ZHU Ren-fa, HE Yong,CHEN Shi-yun, SHAO Guo-quan ( 1. Department of Chemical and Materials Engineering, Hefei University, Hefei 230022 ; 2. Hefei Huijia Chemical Sci & Tech Co. ,LTD,Hefei 230051 )
Abstract:Aim To synthesize the anticaneer intermediate 1,2,3-O-triaeetyl-5-deoxy-D-Riboturanose. Method 5'-iodo-6-hydroxy-9-β-D-purine nueleoside was obtained by using inosine as the starting material by the reaction of iodation, after hydrogenolysis obtained 5 '- deoxy-6-hydroxy-9-β-D-purine nueleoside, 1,2,3-O-triaeetyl-5-deoxy -D-riboturanose was synthesized with acetylation in 3 steps, Result The anticancer intermediate 1,2,3-O-triacetyl-5-deoxy-D-riboturanose was synthesized by using inosine as the starting material in 3 steps. Conclusion The starting material is very cheap and easy to get, the reaction conditions are moderate and the operation is convenient, and the total yield is 38.0%. This method is suitable for industrial production.
Keywords:1  2  3-O-triacetyl-5-deoxy-D-riboturanose  capecitabine  chemical synthesis  antitumor
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