First synthesis of BU-4664L

Yusuke Takahashi, Takafumi Hirokawa, Mai Watanabe, Satomi Fujita, Yusuke Ogura, Masaru Enomoto, Shigefumi Kuwahara

Research output: Contribution to journalArticlepeer-review

6 Citations (Scopus)


The first synthesis of BU-4664L, an actinomycte-produced N-farnesylated dibenzodiazepinone with important biological activities, has been achieved in 18% overall yield from a known benzoic acid derivative by a nine-step sequence that involves an intramolecular Buchwald-Hartwig coupling of a sterically demanding bromo amine intermediate to install the unique tricyclic ring system.

Original languageEnglish
Pages (from-to)5670-5672
Number of pages3
JournalTetrahedron Letters
Issue number41
Publication statusPublished - 2015 Oct 7


  • Alkaloid
  • Antitumor
  • BU-4664L
  • Buchwald-Hartwig reaction
  • Diazepinomicin

ASJC Scopus subject areas

  • Biochemistry
  • Drug Discovery
  • Organic Chemistry


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