1,2,3-O-三乙酰基-5-脱氧核糖的合成工艺研究

Research of synthesis of 1,2,3-O-triacetyl-5-deoxy-D-riboturanose

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。

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.