摘要
拉米夫定是新一代的嘧啶核苷类抗病毒药物,可通过降低乙型肝炎病毒(HBV)依赖RNA的DNA多聚酶生物活性,明显抑制HBV-DNA的合成,具有作用强、安全、不良反应少等特点,是治疗不同类型的乙型病毒性肝炎的新选择。一般的化学合成方法存在异构体拆分困难,如果在合成过程中引入薄荷醇作为手性拆分试剂,可直接得到旋光性的拉米夫定,适合工业化生产。对光学纯拉米夫定的合成及前景进行了综述。
Lamivudine is a typical antivius agent of pyrimidine nucleoside.It inhibits the DNA synthesis of HBV via decreasing the bio-activity of DNA polymerase that depended on RNA.It may be a new choesement in treatment of all kinds of hepatitis B.But because of different spatial structure,there are two optical isomers： L（-）sddc is damaged easily by dcyd dehydrogenase,while L（-）sddc can antagonize dcyd dehydrogenase,is metabolized to lamivudine phosphate in infected hepatocytes and normal hepatocytes, which is the active form of lamivudine. Isomer split is different in normal chemical synthesis methods. If piperitol is used as chiral reagent,optieity lamivudine can he synthesized directly,which is useful in industrialization. The latest research in lamivudine, including its synthesis and application future are reviewed in this study.
出处
《云南化工》
CAS
2009年第6期33-35,共3页
Yunnan Chemical Technology
