克拉霉素的合成进展.pdfVIP

2002 年第 22 卷 有 机 化 学 Vol . 22 , 2002 第 12 期 , 951～963 Chinese Journal of Organic Chemistry No . 12 , 951～963 ·综述与进展 · 克拉霉素的合成进展 孙京国　　梁建华 　　邓志华 　　姚国伟 (北京理工大学生命科学与技术学院　北京 100081) 摘要 　克拉霉素属大环内酯类抗生素 ,是第二代红霉素产品 ,其抗菌谱广 ,抗菌活性高 ,药代动力性能好 ,在国内外 受到广泛重视 ,有着极其重要的应用和发展前景. 对克拉霉素研究的起源与发展 、研制历程 、合成过程中6羟基甲基 化选择性 、活泼基团的保护与脱保护 、各种克拉霉素合成工艺路线以及最新合成方法进行了较为详细的综述. 关键词 　克拉霉素 ,合成 ,综述 Progress in Synthesis of Clarithromycin SUN , JingGuo 　　L IAN G , JianHua 　　DEN G , ZhiHua 　　YAO , GuoWei ( ) School of L fi e Science and Technology , B eij ing Institute of Technology , B eij ing 100081 Abstract 　Clarithromycin (6methylerythromycin A , 1 ) is one of the most important macrolide antibiotics. As the second generation of erythromycin , it is a broadspectrum antibiotic with strong antibacterial activity and more favorable pharmacokinetic behavior . It has been attracted much attention and shows a bright future in the application and development . The present review describes its synthesis and development , including its discov ery , the arts of selective 6OHmethylation synthesis , various techniques of introduction and elimination of the protective group , diverse routes of clarithromycin preparation and latest synthetic techniques. Key word 　clarithromycin , synthesis , review ( ) )