Efficient synthesis of ESI-09, a novel non-cyclic nucleotide EPAC antagonist

Haijun Chen, Chunyong Ding, Christopher Wild, Huiling Liu, Tianzhi Wang, Mark A. White, Xiaodong Cheng, Jia Zhou

Research output: Contribution to journalArticle

27 Scopus citations

Abstract

A concise and efficient synthetic approach to producing a novel non-cyclic nucleotide EPAC antagonist ESI-09 and its new analogs is reported. Key features of the synthesis include a mild and reliable one-pot procedure for an isoxazole synthon, as well as a modified one-pot protocol for the cyanomethyl ketone key intermediate. The synthesis requires inexpensive starting materials and only three linear steps for the completion in a total yield of 53%.

Original languageEnglish (US)
Pages (from-to)1546-1549
Number of pages4
JournalTetrahedron Letters
Volume54
Issue number12
DOIs
StatePublished - Mar 20 2013

Keywords

  • Cyanomethyl ketone
  • EPAC antagonist
  • ESI-09
  • Isoxazole
  • Modified Kowalski's protocol

ASJC Scopus subject areas

  • Biochemistry
  • Drug Discovery
  • Organic Chemistry

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