Total Synthesis and Bioactivity Studies of Fungal Metabolite (-)-TAN-2483B

Org Lett. 2020 Dec 18;22(24):9427-9432. doi: 10.1021/acs.orglett.0c03303. Epub 2020 Nov 24.

Abstract

The first total synthesis of (-)-TAN-2483B, a fungal metabolite possessing a densely functionalized furo[3,4-b]pyran-5-one framework, is achieved in 14 steps from d-mannose. Generation of the 2,6-trans-pyran is by cyclopropane ring expansion followed by α-selective alkynylation. Julia-Kocienski olefination introduces the E-propenyl side chain. Alkyne functionalization and carbonylation stereoselectively establish the bicyclic core of (-)-TAN-2483B. Inhibition of kinases Btk and Bmx, bacterial priority pathogens, and cytokine production in splenocytes indicates promising therapeutic potential.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cyclopropanes / chemistry*
  • Fungi / chemistry
  • Fungi / metabolism*
  • Lactones / chemical synthesis*
  • Lactones / chemistry
  • Molecular Structure
  • Pyrans / chemical synthesis*
  • Pyrans / chemistry
  • Stereoisomerism

Substances

  • Cyclopropanes
  • Lactones
  • Pyrans
  • TAN-2483B
  • cyclopropane