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 .
Clarithromycin (6-methylerythromycin A, 1) is one of the most important macrolide antibiotics - As the second generation of erythromycin, it is a broad-spectrum 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 discovery, the arts of selective 6-OH-methylation synthesis, various techniques of introduction and elimination of the protective group, diverse routes of clarithromycin preparation and latest synthetic techniques.
出处
《有机化学》
SCIE
CAS
CSCD
北大核心
2002年第12期951-963,共13页
Chinese Journal of Organic Chemistry
基金
国家经贸委技术创新 (No .O1BK 0 0 9)项目
