奎奴普丁的合成 |
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引用本文: | 赵传猛,裘鹏程,肖立,尹明星,张福利.奎奴普丁的合成[J].中国医药工业杂志,2012,43(6):401-404. |
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作者姓名: | 赵传猛 裘鹏程 肖立 尹明星 张福利 |
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作者单位: | 1. 中国医药工业研究总院上海医药工业研究院,创新药物与制药工艺国家重点实验室,上海200040 2. 浙江海正药业股份有限公司,浙江台州,318000 |
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基金项目: | 上海市科技人才计划项目(10XD1422800) |
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摘 要: | 普那霉素Ⅰ包括主成分普那霉素ⅠA和次成分普那霉素ⅠB、普那霉素ⅠC.粗品经甲基化反应将普那霉素ⅠB转化为普那霉素ⅠA,纯化后经Mannich反应和消除反应制得5δ-亚甲基普那霉素ⅠA(3),3与(S)-3-奎宁环硫醇反应得抗感染药奎奴普丁,总收率约37%(以普那霉素ⅠA计).
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关 键 词: | 奎奴普丁 普那霉素 甲基化 合成 纯化 抗感染药 |
Synthesis of Quinupristin |
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Authors: | ZHAO Chuanmeng QIU Pengcheng XIAO Li YIN Mingxing ZHANG Fuli |
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Institution: | 1(1.State Key Lab.of New Drug and Pharmaceutical Process,Shanghai Institute of Pharmaceutical Industry,China State Institute of Pharmaceutical Industry,Shanghai 200040;2.Zhejiang Hisun Pharmaceutical Co.,Ltd.,Taizhou 318000) |
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Abstract: | Pristinamycin Ⅰ,including pristinamycinⅠA,pristinamycinⅠB and pristinamycinⅠC,was treated by methylation,in order to convert pristinamycinⅠB to pristinamycinⅠA,then followed by Mannich reaction and elimination to give 5δ-methylenepristinamycinⅠA(3),which was subjected to reaction with(S)-3-mercaptoquinuclidine to obtain anti-infective agent quinupristin with an overall yield of about 37%(based on pristinamycinⅠA). |
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Keywords: | quinupristin pristinamycin methylation synthesis purification anti-infective agent |
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