Expedient Entry to 1-Aminoadamantane Derivatives via Aza-Prins Cyclization of 7-Methylenebicyclo[33.1]nonan-3-one Oximes

Tetsuya Kuga, Yusuke Sasano, Masaki Tomizawa, Masatoshi Shibuya, Yoshiharu Iwabuchi

Research output: Contribution to journalArticlepeer-review

3 Citations (Scopus)

Abstract

An efficient synthesis of 1-aminoadamantane (amantadine) derivatives is described. This synthesis features acid-promoted aza-Prins cyclization of 7-methylenebicyclo[3.3.1]nonan-3-one oximes, which are readily prepared from 1,3-adamantanediol via a Grob fragmentation and the subsequent oximation, to give various 3-substituted 1-(alkoxyamino)adamantanes. After the reduction of alkoxyamines, not only 3-substituted 1-aminoadamantanes, but also chiral 2,5-disubstituted derivatives were obtained in good yields.

Original languageEnglish
Article numberss-2017-f0782-op
Pages (from-to)1820-1826
Number of pages7
JournalSynthesis (Germany)
Volume50
Issue number9
DOIs
Publication statusPublished - 2018 May 2

Keywords

  • 1-(alkoxyamino)-adamantanes
  • 1-aminoadamantanes
  • amantadine
  • aza-Prins reaction
  • oxime

ASJC Scopus subject areas

  • Catalysis
  • Organic Chemistry

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