摘要
综述了近年来主要的核苷类抗乙肝病毒药物的研究进展及其合成方法。现有的核苷类药物主要包括了拉米夫定、阿德福韦酯、恩替卡韦,它们对于乙肝病患者都具有一定疗效。对于拉米夫定的合成,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,整个反应的原料有来源,适合工业化生产。阿德福韦酯最早由美国Starrett等人合成并公开的。目前合成阿德福韦酯的主要方法,都是以腺嘌呤为起始原料,所不同的是在进行侧链的合成时有所改变。此外,还介绍了恩替卡韦的合成方法。
The present article reviews the new advances of nueleoside drugs against chronic hepatitis B, and sums up the kinds of nueleoside drugs against chronic hepatitis B. Specially, synthesis of some nueleoside drugs including lamivudine, adefovir and entecavir are disclosed. In order to synthesize lamivudine, the introduction of chiral menthol as the chiral disassemble reagent may directly obtain optical rotation. The entire raw material source is not difficult, and the process is suitable to the industrial production. At present, the main synthesis method of adefovir synthesized and published firstly by Starrett et al is based upon the adenine as raw material, what is different is the synthesis of the side chain. Besides, this article involves the preparation of entaeavir.
出处
《精细化工中间体》
CAS
2008年第2期16-22,共7页
Fine Chemical Intermediates
