硼氢化立体选择性还原制备拉米夫定的研究

On the Stereo-selective Reduction and Preparation of Lamivudine through Borohydride

在对核苷类抗病毒药物拉米夫定的制备进行文献综述的基础上,提出一条立体选择硼氢化还原的合成路线合成了拉米夫定.反应中形成的六元环过渡态结构有效抑制消旋化,使得反应过程工艺简单,产品纯度好,收率高,完全符合作为原料药的使用要求.

Basing on the literature about the preparation of nucleoside antiviral drug Lamivudine, the paper provided a stereo-selective synthetic route by borohydride as the reducing agent. The formed six-membered ring transition state structure effectively inhibited the racemization, it made the reaction process have the advantages of simple process, pure product and high yield, which completely accorded with the usage requirements as the crude drug.