摘要
拉米夫定是具有抗HIV和抗HBV生物活性的2′-脱氧核苷酸类似物.以溴代乙酸、乙醛酸为不同的起始原料合成中间体二羟基乙醛酸薄荷酯,比较两种工艺发现:乙醛酸为原料的工艺路线较短,费用较低;二羟基乙醛酸薄荷酯与2,5-二羟基-1,4-二噻烷成环反应、氯化、偶联、还原反应可以合成拉夫米定.同时,改进了合成和分离工艺,总收率达到22.5%.改进后的工艺路线较短,操作简便,适合于工业化生产.
Lamivudine is a 2＇-deoxy nucleoside analogue with a biological importance of an anti-HIV and anti-HBV.On the comparison of two technologies that the intermediate menthyl dihydroxy glycoxylate was synthesized with bromoacetic acid or glycoxylic acid as a different raw material,the synthetic technology is discovered shorter steps and lower cost with glycoxylic acid as a raw material.Menthyl dihydroxy glycoxylate was reacted to cyclization with 2,5-dihydroxy-1,4-dithiane,subsequent chlorinated,coupled,and reduced to obtain lamivudine.Meanwhile,the synthesis and separation technology was improved,and the overall yield is reached 22.5%.The improved technology herein is applicable to industrial production as the advantage of shorter steps,concise and practical operation.
出处
《湘潭大学自然科学学报》
CAS
CSCD
北大核心
2010年第4期78-83,共6页
Natural Science Journal of Xiangtan University
基金
湖南省自然科学基金项目(05JJ40054)
第二批湖南省大学生研究型学习与创新实验计划项目(批准号:No.87)
关键词
拉米夫定
抗病毒药物
合成
lamivudine
antiviral agents
synthesis
