施翔,邓瑜,鞠涛,等.海洋细菌代谢物Pelagiomicin-A的全合成[J].中国海洋药物,2023,42(5):41-46.
海洋细菌代谢物Pelagiomicin-A的全合成
Total synthesis of pelagiomicin-A
投稿时间：2022-03-12  修订日期：2022-04-22
DOI：10.13400/j.cnki.cjmd.2023.05.008
中文关键词:  Pelagiomicin-A  全合成  海洋细菌  代谢物
English Keywords:Pelagiomicin-A  Total synthesis  Marine Bacteria  Metabolites
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作者单位E-mail
施翔 东南大学 101102029@seu.edu.cn 
邓瑜 东南大学 220184914@seu.edu.cn 
鞠涛 上海同联制药有限公司 ju0826@sina.com 
孙玥* 安徽农业大学 yuesun@ahau.edu.cn 
鞠采儿 沈阳药科大学  
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中文摘要:
      目的 为了实现海洋细菌代谢物pelagiomicin-A 系统的活性和药效学研究,开发其全合成方法。方法 以简单易得的3-溴-4-甲氧基苄醇为起始原料,通过烷基化、环合、格式等经典反应,完成了pelagiomicin-A的制备。结果 通过12步汇聚式反应成功得到目标化合物pelagiomicin-A,总收率为15.2 %,ee >98.8%。
English Summary:
      Objective To achieve a comprehensive activity and pharmacodynamic study of the marine bacterial metabolite pelagiomicin-A, a total synthesis method was achieved. Methods The preparation of pelagiomicin-A was accomplished by easy-to-operate classical reactions such as alkylation reaction, cycloaddition reaction and Grignard reaction using 3-bromo-4-methoxybenzyl alcohol as the starting material. Results Pelagiomicin-A was successfully obtained by a 12-step convergent reaction with a total yield of 15.2%, ee >98.8%.
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