9 抗トリパノソーマ活性を有するマングロマイシン類の単離、構造決定ならびに不斉全合成 (口頭発表の部)

DOI

書誌事項

タイトル別名
  • 9 Mangromicin A with Potent Antitrypanosomal Activity; Isolation, Structure Elucidation and Asymmetric Total Synthesis

抄録

Two new cyclopentadecane antibiotics, named mangromicins A and B, were separated out from the culture broth of Lechevalieria aerocolonigenes K10-0216. The chemical structures of the two novel compounds were elucidated by instrumental analyses, including various NMR, MS and X-ray crystallography. Mangromicins A and B consist of cyclopentadecane skeletons with a tetrahydrofuran unit and a 5,6-dihydro-4-hydroxy-2-pyrone moiety. Mangromicins A and B showed in vitro antitrypanosomal activity with IC50 values of 2.4 and 43.4 μg/ml, respectively. An enantioselective total synthesis of (+)-mangromicin A has also been accomplished. The tetrahydrofuran ring of mangromicin A, possessing a tetrasubstituted carbon center, was constructed by Mukaiyama-type vinylogous alkylation via a cyclic oxocarbenium intermediate derived from a γ-hydroxy ketone with ideal stereoselectivity, and the 4-hydroxydihydropyrone scaffold was generated via Dieckmann condensation at a late stage of the total synthesis. The reliable asymmetric synthesis of (+)-mangromicin A has revealed the absolute configuration of naturally occurring mangromicin A.

収録刊行物

詳細情報 詳細情報について

  • CRID
    1390004222620946176
  • NII論文ID
    130007906363
  • DOI
    10.24496/tennenyuki.59.0_49
  • ISSN
    24331856
  • 本文言語コード
    ja
  • データソース種別
    • JaLC
    • CiNii Articles
  • 抄録ライセンスフラグ
    使用不可

問題の指摘

ページトップへ