| 4″-烷氧基-1,1′:4′,1″-三联苯-4-羧酸的合成 |
| 投稿时间：2010-04-28 修订日期：2010-05-14 点此下载全文 |
| 引用本文：刘红明,秦烨,姚建忠,盛春泉,缪震元,张万年.4″-烷氧基-1,1′:4′,1″-三联苯-4-羧酸的合成[J].药学实践杂志,2010,28(6):414~417,459 |
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| 基金项目:国家自然科学基金(30772674、30930107);上海市重点学科建设基金(B906)资助项目 |
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| 中文摘要:目的:制备用于全合成新型卡泊芬净(caspofungin)类环六脂肽抗真菌剂的关键脂肪酸侧链4″-烷氧基-1,1′:4′,1″-三联苯-4-羧酸(1)。方法:以4′-溴-4-羟基-1,1′-联苯(2)为原料,经羟基烃化、溴金属锂交换及硼酸三异丙酯加成异丙酯酸水解、4-碘苯甲酸甲酯的Suzuki偶联及甲酯碱水解4步反应制备目标化合物。结果:以79.5%-93.1%的总收率成功合成了目标化合物1a-1e,其结构经电喷雾质谱(ESI-MS)和氢谱(1H NMR)确证。其中,化合物1a和1d为首次报道。结论:该合成路线具有反应时间短、操作简便及收率高等优点。 |
| 中文关键词:4″-烷氧基-1,1′,′1″-三联苯-4-羧酸 合成 4′-溴-4-羟基-1,1′-联苯 Suzuki偶联 |
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| Synthesis of 4″-alkoxy-1,1′:4′,1″-terphenyl-4-carboxylic acids |
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| Abstract:Objective To prepare 4″-alkoxy-1,1′:4′,1″-terphenyl-4-carboxylic acids(1),the key fatty acid chain which is pharmaceutical intermediates for the total synthesis of novel cyclohexalipopeptide antifungal agents such as Caspofungin analogs.Methods Starting from 4′-bromo-4-hydroxy-1,1′-biphenyl(2),Results target compounds 1a-1e were prepared via hydrocarbylation,halogen-mental exchange followed by condensation with triisopropyl borate and acid hydrolysis. |
| keywords:4″-alkoxy-1,1′′,1″-terphenyl-4-carboxylic acid synthesis 4′-bromo-4-hydroxy-1,1′-biphenyl Suzuki coupling |
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