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

Research output: Contribution to journalArticle

62 Citations (Scopus)

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.
LanguageUndefined/Unknown
Pages859-867
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
Bagley, Mark C. ; Hughes, David D. ; Lubinu, M. Caterina ; Merritt, Eleanor A. ; Taylor, Paul H. ; Tomkinson, Nicholas C. O. / Microwave-assisted synthesis of pyrimidine libraries. In: QSAR and Combinatorial Science. 2004 ; Vol. 23, No. 10. pp. 859-867.
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Bagley, MC, Hughes, DD, Lubinu, MC, Merritt, EA, Taylor, PH & Tomkinson, NCO 2004, 'Microwave-assisted synthesis of pyrimidine libraries' QSAR and Combinatorial Science, vol. 23, no. 10, pp. 859-867. https://doi.org/10.1002/qsar.200420044

Microwave-assisted synthesis of pyrimidine libraries. / Bagley, Mark C.; Hughes, David D.; Lubinu, M. Caterina; Merritt, Eleanor A.; Taylor, Paul H.; Tomkinson, Nicholas C. O.

In: QSAR and Combinatorial Science, Vol. 23, No. 10, 2004, p. 859-867.

Research output: Contribution to journalArticle

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AU - Bagley, Mark C.

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AU - Tomkinson, Nicholas C. O.

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