有机化学 ›› 2019, Vol. 39 ›› Issue (10): 2936-2940.DOI: 10.6023/cjoc201907024 上一篇    下一篇

研究简报

Pulchrol和Pulchral的合成研究

郭冬冬a, 张武霞a, 高文梅a, 郭晓迪a, 王永强b*()   

  1. a 山西农业大学文理学院 山西太谷 030801
    b 西北大学化学与材料科学学院 西安 710069
  • 收稿日期:2019-07-17 修回日期:2019-08-20 发布日期:2019-09-05
  • 通讯作者: 王永强 E-mail:wangyq@nwu.edu.cn
  • 基金资助:
    国家自然科学基金(31800678);山西省青年基金(201801D221062);山西省青年基金(201801D221063);山西省优秀博士来晋工作奖励(SXYBKY201737);山西省优秀博士来晋工作奖励(SXYBKY201706);山西农业大学科技创新基金(Nos. 2017YJ38);山西农业大学科技创新基金(2017YJ41)

Total Synthesis of Pulchrol and Pulchral

Guo, Dongdonga, Zhang, Wuxiaa, Gao, Weimeia, Guo, Xiaodia, Wang, Yongqiangb*()   

  1. a College of Arts and Sciences, Shanxi Agricultural University, Taigu 030801, Shanxi
    b Department of Chemistry &Materials Science, Northwest University, Xi'an 710069;
  • Received:2019-07-17 Revised:2019-08-20 Published:2019-09-05
  • Contact: Wang, Yongqiang E-mail:wangyq@nwu.edu.cn
  • Supported by:
    Project supported by the National Natural Science Foundation of China(31800678);the Science and Technology Research Project in ShanXi Province(201801D221062);the Science and Technology Research Project in ShanXi Province(201801D221063);the Shanxi Excellent Doctor Grant Award(SXYBKY201737);the Shanxi Excellent Doctor Grant Award(SXYBKY201706);the Science and Technology Innovation Project of Shanxi Agricultural University(Nos. 2017YJ38);the Science and Technology Innovation Project of Shanxi Agricultural University(2017YJ41)

以廉价的对苯二酚和4-甲基苯甲酸为原料, 以钯催化芳烃羧酸与芳基溴化物的分子内脱羧偶联为关键反应, 合成了具有抗疟原虫活性的天然产物pulchrol和pulchral, 总收率分别为14%和11%. 该合成为进一步研究构效关系提供了基础.

关键词: 天然产物, 全合成, 交叉偶联, pulchrol, pulchral

The total synthesis of natural products pulchrol and pulchral with antiprotozoan activity was reported, starting from the cheap hydroquinone and 4-methylbenzoic acid and using palladium-catalyzed intramolecular decarboxylation coupling reaction of arene carboxylic acids with aryl bromides as the key reaction. This method provides an opportunity for further study of the structure-activity relationship.

Key words: natural product, total synthesis, cross-coupling, pulchrol, pulchral