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Jietacins with potent nematocidal activity; efficient isolation of novel analogs and divergent total synthesis of jietacin A, B, C, and D

Tetrahedron, ISSN: 0040-4020, Vol: 71, Issue: 14, Page: 2149-2157
2015
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Article Description

Jietacin compounds are known to display potent nematocidal activity being 10-fold more active against the pine wood nematode ( Bursaphelenchus lignicolus ) than avermectin B1a. They consist of a unique functional vinylazoxy group. Herein, we disclose not only the isolation of novel analogs (jietacin C and D) but also a divergent and a 7-step total synthesis for jietacin A, B, C, and ( S and R ) D in 30–36% overall yield, incorporating reductive hydrazination, regioselective azoxy formation, and C–C bond formation via acylation using Grignard reagents in the presence of vinylazoxy moiety at the final stage. In addition, we evaluated the nematocidal activity of jietacin A–D and synthetic intermediates against Caenorhabditis elegans as a model nematode.

Bibliographic Details

Akihiro Sugawara; Masahiko Kubo; Takuji Nakashima; Tomoyasu Hirose; Noriaki Tsunoda; Kyoichi Yahagi; Yukihiro Asami; Takeshi Yamada; Kazuro Shiomi; Yōko Takahashi; Satoshi Ōmura; Toshiaki Sunazuka

Elsevier BV

Biochemistry, Genetics and Molecular Biology; Pharmacology, Toxicology and Pharmaceutics; Chemistry

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