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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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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