2-Fluoropyrimidine as an efficient reagent in solid-phase synthesis of N-aryl- and N-alkyl-N-pyrimidin-2-ylamines

Christoph Gibson, Horst Kessler

Research output: Contribution to journalArticlepeer-review

9 Scopus citations

Abstract

Mild and efficient reaction conditions were developed for the solid- phase synthesis of N-aryl- and N-alkyl-N-pyrimidin-2-ylamines. 2- Fluoropyrimidine in the presence of DIEA showed suitable properties for reactions with resin-bound alkylamines at room temperature. Since anilines proved to be inert under these conditions, an alternative approach was developed using BF3·Et2O as a potent catalyst for the reaction of anilines with 2-fluoropyrimidine.

Original languageEnglish
Pages (from-to)1725-1728
Number of pages4
JournalTetrahedron Letters
Volume41
Issue number11
DOIs
StatePublished - 11 Mar 2000

Keywords

  • Catalysis
  • Combinatorial chemistry
  • Pyrimidines
  • Solid-phase synthesis

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