Stereoselective synthesis of (-)-8-epi-swainsonine starting with a chiral aziridine

  • Lee, Baeck Kyoung
  • Choi, Hwan Geun
  • Roh, Eun Joo
  • Lee, Won Koo
  • Sim, Taebo
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초록

An efficient synthesis of (-)-8-epi-swainsonine, starting from a commercially available 1-(R)-alpha-methylbenzylaziridine-2-methanol, was developed. The synthetic route utilizes stereocontrolled Sharpless asymmetric dihydroxylation governed by AD-mix-beta followed by an aziridine ring opening-cyclization sequence to generate the five membered N-heterocyclic ring system present in the bicyclic target. A subsequent stereoselective allylation and piperidine ring forming cyclization then produced a precursor that was converted into (-)-8-epi-swainsonine. (c) 2012 Elsevier Ltd. All rights reserved.

키워드

Indolizidine alkaloids(-)-8-Epi-swainsonineTotal synthesisAziridineNatural productRING-CLOSING METATHESISASYMMETRIC SYNTHESESSWAINSONA-CANESCENSNATURAL OCCURRENCEALPHA-MANNOSIDASE(-)-SWAINSONINEINHIBITIONALKALOIDSANALOGSDIHYDROXYLATION
제목
Stereoselective synthesis of (-)-8-epi-swainsonine starting with a chiral aziridine
저자
Lee, Baeck KyoungChoi, Hwan GeunRoh, Eun JooLee, Won KooSim, Taebo
DOI
10.1016/j.tetlet.2012.11.087
발행일
2013-02-06
유형
Article
저널명
Tetrahedron Letters
54
6
페이지
553 ~ 556