2’-脱氧腺苷的合成

Synthesis of 2'-deoxyadenosine

以腺嘌呤(Ⅰ)和1-乙酰氧基-3,5-二(对甲基苯甲酰基)-2-脱氧核糖(Ⅱ)为原料,先将腺嘌呤进行硅醚保护,然后与Ⅱ催化缩合生成带保护基的2’-脱氧腺苷,脱保护基,得到-βD-2’-脱氧腺苷。考察了反应物(Ⅰ)和(Ⅱ)的摩尔比、催化剂的用量及反应温度对2’-脱氧腺苷收率的影响。结果表明,最佳反应条件为:(Ⅰ)∶(Ⅱ)(摩尔比)=1∶1,催化剂用量为0.54%,反应温度为20℃时,2’-脱氧腺苷的总收率可达65%。

Abstract ：2＇ -Deoxyadenosine was synthesized from adenosine（I） and 1-acetoxy-3,5-di （p-methyl-benzo- yl）-2-deoxy-ribose（Ⅱ）. Adenosine was silyiated and condensated with raw charge （Ⅱ） to synthesized 2＇- deoxyadenosine with protective group in the presence of special catalyst, then the protective group was eliminated in a controlling condition. The influences of other conditions including the mole ratio of reactant （ I ） to （Ⅱ） and amount of catalyst, temperature on yield of products were also discussed. Results showed the mole ratio of （ I ） to （ Ⅱ ） was 1 ： 1, the amount of catalyst was 0.54%, the optimal reaction temperature was 20℃, the yield of 2＇ -deoxyadenosine achieved 65%.