3-脱克拉定糖-3-酮基-6-O-甲基-10,11-脱氢-12-O-咪唑酰基-2′-苯甲酰基红霉素A的合成  

Studies on the synthesis of 3-ketolide-6-O-methyl-2′-benozoic-10,11-dehydide-12-acyl imidazoyl erythromycin A

作　　者：王翀[1] 郑忠辉[1] 

机构地区：[1]山东新华制药股份有限公司,淄博255005

出　　处：《齐鲁药事》2006年第10期617-618,共2页qilu pharmaceutical affairs

摘　　要：目的合成制备泰利霉素的关键中间体。方法以3-脱克拉定糖-3-酮基-6-O-甲基-2′-苯甲酰基红霉素A为起始原料,经过甲磺酯化、碱消除、咪唑酰基化三步成功地合成关键中间体3-脱克拉定糖-3-酮基-6-O-甲基-10,11-脱氢-12-O-咪酰基-2′-苯甲酰基红霉素A,并进行了工艺改进。结果与结论新的合成工艺与未改进时相比,总收率提高10%,为科研和工业化生产奠定基础。OBJECTIVE Studies on the synthesis of the key intermediate of Telithromyin. METHODS 3-ketolide-6-O- methyl-2＇-benozoic-10,11-dehydide-12-acyl imidazoyl erythromycin A was synthesized through methylsulfication, elimination and imidazoylacylation RESULTS and CONCLUSION Comparing to the old craft yield, the total recovery enhanced 10% and the improved procedure was convenient to Industrialized product and research.

关 键 词：泰利霉素 关键中间体 氧化 合成 

分 类 号：TQ460.31[化学工程—制药化工]