| 第 36 卷第 2 期 |  | Vol. 36 No. 2 | | 2006 年 4 月 | Apr 2006 |
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所屬欄目：醫藥及中間體
橋紅霉素亞胺的合成 |
| 梁群; 陳士清; 陳吉人(湖北百科藥業(yè)股份有限公司; 湖北荊門(mén)) |
| 摘 要：以紅霉素肟為起始原料,經(jīng)三乙�；�、橋化、還原、乙�；膫�(gè)步驟合成橋紅霉素亞胺,總收率28%。橋紅霉素亞胺用于生產(chǎn)新型抗生素類(lèi)藥物——橋紅霉素,它是在紅霉素內酯環(huán)結構上脫掉cladinosesugar,并將紅霉素內酯環(huán)上6,11位相連,成為全新的紅霉素衍生物。此藥不但克服了該類(lèi)抗生素藥物的耐藥性,而且具有較好的抗菌活性。 |
| 關(guān)鍵詞：橋紅霉素亞胺; 大環(huán)內酯類(lèi)抗生素; 合成 |
| 中圖分類(lèi)號：TQ465.5 文獻標識碼：A 文章編號：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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