| 第 36 卷第 2 期 |  | Vol. 36 No. 2 | | 2006 年 4 月 | Apr 2006 |
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所属栏目：医药及中间体
桥红霉素亚胺的合成 |
| 梁群; 陈士清; 陈吉人(湖北百科药业股份有限公司; 湖北荆门) |
| 摘 要：以红霉素肟为起始原料,经三乙酰化、桥化、还原、乙酰化四个步骤合成桥红霉素亚胺,总收率28%。桥红霉素亚胺用于生产新型抗生素类药物——桥红霉素,它是在红霉素内酯环结构上脱掉cladinosesugar,并将红霉素内酯环上6,11位相连,成为全新的红霉素衍生物。此药不但克服了该类抗生素药物的耐药性,而且具有较好的抗菌活性。 |
| 关键词：桥红霉素亚胺; 大环内酯类抗生素; 合成 |
| 中图分类号：TQ465.5 文献标识码：A 文章编号：1009-9212(2006)02-0021-03 |
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| Synthesis of Bridged Imine Acetamide |
| LIANG Qun; CHEN Shi-qing; CHEN Ji-ren（Hubei Biocause Pharmaceutical Co.; Ltd.; Jingmen 448000; China） |
| Abstract：Bridged imine acetamide was synthesized via the reactions such as triacetylation,bridge formation,reduction and acetylation,using Ery A oxime as the starting material. The total yield of the product was 28%. Bridged imine acetamide was used to produce a new type of antibiotic derivatives from macrolid via removing cladinose sugar from macrolid and joining 6 and 11 position on macrolid ring. It not only overcame the drug tolerance,but also enhanced the antibacterial activity. |
| Key words：bridged imine acetamide; macrolid antibiotic; synthesis |
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收稿日期：2005-10-17
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