Enantioselective Synthesis of (+)-Hippolide J and Reevaluation of Antifungal Activity.

Enantioselective Synthesis of (+)-Hippolide J and Reevaluation of Antifungal Activity.
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(+)-Hippolide J的对映选择性合成及其抗真菌活性的再评价

DOI:
10.1021/acs.orglett.0c02979
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发表时间:
2020-10-02
期刊:
影响因子:
5.2
通讯作者:
Brown MK
Brown MK
中科院分区:
化学1区
文献类型:
--
作者:
Guo R;Beattie SR;Krysan DJ;Brown MK

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报道了抗真菌剂(+)-hippolide J的合成方法。通过实施对映异构化/[2 + 2]-环加成序列使天然产物的快速组装成为可能。由于该路线的简单性,在单程中制备>100 mg的天然产物。然而,hippolide J的抗真菌试验证实,它对几种真菌菌株没有活性,与分离报告相反。
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.
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