对映选择性合成 (+)-海鞘素 J 和抗真菌活性的再评价。
Enantioselective Synthesis of (+)-Hippolide J and Reevaluation of Antifungal Activity.
机构信息
Indiana University, Department of Chemistry, 800 East Kirkwood Avenue, Bloomington, Indiana 47405, United States.
University of Iowa, Carver College of Medicine, Departments of Pediatrics and Microbiology/Immunology, 200 South Grand Avenue, Iowa City, Iowa 52242, United States.
出版信息
Org Lett. 2020 Oct 2;22(19):7743-7746. doi: 10.1021/acs.orglett.0c02979. Epub 2020 Sep 24.
Abstract
A synthesis of the reported antifungal agent (+)-hippolide J is presented. The rapid assembly of the natural product was enabled through implementation of an enantioselective isomerization/[2 + 2]-cycloaddition sequence. Due to the simplicity of the route, >100 mg of the natural product were prepared in a single pass. Anitfungal assays of hippolide J, however, confirmed that it showed no activity against several fungal strains, contrary to the isolation report.
摘要
现报道抗真菌剂（+）-hippolide J 的全合成。通过实施对映选择性异构化/[2 + 2]-环加成序列，能够快速组装该天然产物。由于路线简单，一次通过即可制备超过 100 毫克的天然产物。然而，hippolide J 的抗真菌试验证实，与分离报告相反，它对几种真菌菌株均没有活性。
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