Microwave-assisted synthesis of pyrimidine libraries

Mark C. Bagley, David D. Hughes, M. Caterina Lubinu, Eleanor A. Merritt, Paul H. Taylor, Nicholas C. O. Tomkinson

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Abstract

Di- and trisubstituted pyrimidine libraries are prepd. in good yields by the microwave irradn. of an alkynone R1C≡CCOR2 [R1 = H, Ph; R2 = Ph, 4-MeOC6H4, 3,4-(MeO)2C6H3, etc.] and either an amidine or guanidine at 120-150° in acetonitrile in the presence of sodium carbonate or at 100° after treatment with methanolic sodium methoxide in a sealed tube using a monomodal microwave synthesizer. These rapid and efficient methods often require no chromatog. purifn. and so are appropriate for automated combinatorial methodol. and have been applied in the synthesis of a small library of potentially useful novel ligands for the estrogen receptor based on the pyrimidine template.
Original languageUndefined/Unknown
Pages (from-to)859-867
Number of pages9
JournalQSAR and Combinatorial Science
Volume23
Issue number10
DOIs
Publication statusPublished - 2004

Keywords

  • pyrimidine libraries
  • microwave-assisted synthesis
  • novel ligands

Cite this

Bagley, M. C., Hughes, D. D., Lubinu, M. C., Merritt, E. A., Taylor, P. H., & Tomkinson, N. C. O. (2004). Microwave-assisted synthesis of pyrimidine libraries. QSAR and Combinatorial Science, 23(10), 859-867. https://doi.org/10.1002/qsar.200420044