Syntheses of Biologically Active 2-Arylcyclopropylamines

Shin Miyamura, Kenichiro Itami, Junichiro Yamaguchi*

*Corresponding author for this work

Research output: Contribution to journalReview articlepeer-review

14 Citations (Scopus)


The 2-arylcyclopropylamine (ACPA) motif is often seen in biologically active compounds. This review focuses on the synthesis of biologically active ACPAs and categorizes, by reaction type, the synthetic methods used toward such compounds. 1 Introduction 2 Cyclopropanation Using Diazo Compounds 2.1 Styrene 2.2 Cinnamate 2.3 Vinyl Phthalimide 2.4 Vinyl Acetamide 2.5 Oxazolone 2.6 Diketopiperazine 3 Cyclopropanation Using Ylides 3.1 Cinnamate 3.2 Nitrostyrene 3.3 Oxirane 3.4 Nitroacetate 4 Transformation of Cyclopropanes 4.1 Iodocyclopropane 4.2 Aminocyclopropane 5 Miscellaneous Methods 5.1 Kulinkovich Reaction 5.2 Three-Component Reaction 5.3 Intramolecular Nucleophilic Cyclization 5.4 Intramolecular Mitsunobu Reaction 5.5 Rearrangement from Cyclobutanone 6 Summary.

Original languageEnglish
Article numberss-2016-e0599-r
Pages (from-to)1131-1149
Number of pages19
JournalSynthesis (Germany)
Issue number6
Publication statusPublished - 2017 Mar 15


  • arylcyclopropylamine
  • biologically active compounds
  • cyclopropanes

ASJC Scopus subject areas

  • Catalysis
  • Organic Chemistry


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