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Microwave-assisted synthesis of pyrimidine libraries

Bagley, Mark C. and Hughes, David D. and Lubinu, M. Caterina and Merritt, Eleanor A. and Taylor, Paul H. and Tomkinson, Nicholas C. O. (2004) Microwave-assisted synthesis of pyrimidine libraries. QSAR and Combinatorial Science, 23 (10). pp. 859-867. ISSN 1611-020X

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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.

Item type: Article
ID code: 34249
Notes: M1 - Copyright (C) 2011 American Chemical Society (ACS). All Rights Reserved. CAPLUS AN 2005:40257(Journal)
Keywords: pyrimidine libraries , microwave-assisted synthesis, novel ligands , Chemistry, Organic Chemistry, Drug Discovery, Computer Science Applications
Subjects: Science > Chemistry
Department: Faculty of Science > Pure and Applied Chemistry
Depositing user: Pure Administrator
Date Deposited: 20 Oct 2011 14:15
Last modified: 05 Sep 2014 10:40
URI: http://strathprints.strath.ac.uk/id/eprint/34249

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