制备磷酰胺RNA核糖核苷酸嘌呤的高区域保护

目的:制备磷酰胺RNA核糖核苷酸嘌呤的高区域保护。方法:用一氢磷酰盐的方法来保护RNA甲硅烷基化合成的反应。结果:以鸟苷为原料生成苯氧乙酰胺来保护羟基,合成RNA中间体,通过液相图谱的方法来检验合成的物质。结论:本实验方法是基于二位的羟基是高区域专一的硅烷化作用,为了更有效的使羟基硅烷化用磷酰胺的方法,我们以前是定量的使一氢磷酰脂分裂,没有甲硅烷基的转化,除此之外,相同的方法,高区域专业用阻止硅烷化和磷酰化的方法。

High Yield Protection of Purine Ribonucleosides for Phosphoramidite RNA Sythesis

Objective: To make of high yield protection of purine ribonucleosides for phosphoramidite RNA sythesis. Methods: Base on a reaction which allows concomitant highly regiospecific 2 - silylation and 3 - phosphitylation. Subsequent cleavage of the H - phosphonatd monoester moiety without sily migration provides intermediates ready for phosohitylation by standards methods to give fully protected phosphoramidites. Results: With both nucleosides we use transient protection of the 2, 3diol moiety of the ribonucleosides by reaction with N, N - dimethylformamide dimethylacetal to prevent the small, but potentially troublesome tritylation of the 2 - hydroxyl that otherwise accompanies tritylation of the 5 - hydroxyl. Conclusion:The procedures reported guanosine only in order of introduction of the phenoxyacetyl amino protecting group. Despite the significant progress on use of amino- unprotected monomers in phosphoramidite synthesis, complications remain, and we chose to use amino protection.