| 盐酸沃尼妙林的合成 |
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| 引用本文： | 冯德鑫,李新乐,潘强,王峥,Michael H.CHEN.盐酸沃尼妙林的合成[J].中国医药工业杂志,2010,41(4). |
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| 作者姓名： | 冯德鑫 李新乐 潘强 王峥 Michael H.CHEN |
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| 作者单位： | 北京中牧科技服务有限责任公司,北京,100176 |
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| 摘 要： | 截短侧耳素经苯磺酰化后经1-氨基-2-甲基丙-2-硫醇盐酸盐取代,得到(2.氨基-1,1-二甲基乙基)硫基]乙酸(3aS,4R,5S,6S,8R,9R,9aR,10R)-6-乙烯基十氢-5-羟基-4,6,9,10-四甲基-1-氧代-3a,9-丙醇-3aH-环戊二烯并环辛烯-8-基酯(5).另用D-缬氨酸和乙酰乙酸甲酯反应后,与氯甲酸异丁酯成酸酐,与5成酰胺后用盐酸脱保护,制得抗生素盐酸沃尼妙林,总收率约为64%(以截短侧耳素计).
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| 关 键 词： | 沃尼妙林 截短侧耳素 抗生素 合成 |
Synthesis of Valnemulin Hydrochloride |
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| Authors: | Michael HCHEN |
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| Abstract: | Valnemulin hydrochloride was synthesized by reaction from D-valine with methyl acetoacetate, anhydridisation with isobutyl chloroformate, amidation with (2-amino-l,l-dimethylethyl)thio]acetic acid (3a5,4R,5S,6S,8R,9R,9aR,10R)-6-ethenyldecahydro-5-hydroxy-4,6,9,10-tetramethyl-1-oxo-3a,9-propano-3aH-cyclopentacycloocten-8-yl ester (5) followed by deprotection with hydrochloric acid. Compound 5 was prepared from pleuromutilin by tosylation and substitution with l-amino-2-methylpropane-2-thiol hydrochloride. The overall yield was about 64% (based on pleuromutilin). |
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| Keywords: | valnemulin pleuromutilin antibiotics synthesis |
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