The one-pot solution phase preparation of fused tetrazole-ketopiperazines

T. Nixey, M. Kelly, C. Hulme

Research output: Contribution to journalArticlepeer-review

79 Scopus citations


A novel application of the TMSN3 modified Ugi 4-component reaction is disclosed for the solution phase synthesis of fused tetrazole-ketopiperazine libraries. The reaction of an aldehyde, primary amine, methyl isocyanoacetate and trimethylsilylazide in methanol at reflux affords bicyclic tetrazole-ketopiperazines in good yield. This efficient one step protocol, producing products with three potential diversity points, may be used to generate arrays of biologically relevant small molecules for general and targeted screening. (C) 2000 Elsevier Science Ltd.

Original languageEnglish (US)
Pages (from-to)8729-8733
Number of pages5
JournalTetrahedron Letters
Issue number45
StatePublished - Nov 4 2000

ASJC Scopus subject areas

  • Biochemistry
  • Drug Discovery
  • Organic Chemistry


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