Design and de Novo Synthesis of 6-Aza-artemisinins

Karunakar Reddy Bonepally, Takahisa Hiruma, Haruki Mizoguchi, Kyohei Ochiai, Shun Suzuki, Hideaki Oikawa, Aki Ishiyama, Rei Hokari, Masato Iwatsuki, Kazuhiko Otoguro, Satoshi Omura, Hiroki Oguri

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Abstract

Development of designer natural product variants, 6-aza-artemisinins, enabled us to achieve structural modification of the hitherto unexplored cyclohexane moiety of artemisinin and concise de novo synthesis of the tetracyclic scaffold in just four steps from the modular assembly of three simple building blocks. This expeditious catalytic asymmetric synthetic approach generated lead candidates exhibiting superior in vivo antimalarial activities to artemisinin.

Original languageEnglish
Pages (from-to)4667-4671
Number of pages5
JournalOrganic Letters
Volume20
Issue number15
DOIs
Publication statusPublished - Aug 3 2018
Externally publishedYes

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ASJC Scopus subject areas

  • Biochemistry
  • Physical and Theoretical Chemistry
  • Organic Chemistry

Cite this

Bonepally, K. R., Hiruma, T., Mizoguchi, H., Ochiai, K., Suzuki, S., Oikawa, H., Ishiyama, A., Hokari, R., Iwatsuki, M., Otoguro, K., Omura, S., & Oguri, H. (2018). Design and de Novo Synthesis of 6-Aza-artemisinins. Organic Letters, 20(15), 4667-4671. https://doi.org/10.1021/acs.orglett.8b01987