Convenient preparation of 4-aryl-2-(heteroarylamino)pyrimidines and 4-anilino-2-(heteroarylamino)pyrimidines

A method for the efficient assembly of novel 4-aryl- and 4-anilino-2-(heteroarylamino)pyrimidines via Buchwald–Hartwig N-arylations at elevated temperatures under sealed tube conditions is reported. 4-Aryl-2-anilinopyrimidines and 2,4-dianilinopyrimidines are privileged structures found in many drug...

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Published inTetrahedron letters Vol. 51; no. 25; pp. 3259 - 3262
Main Authors Bliss, Brian I., Ahmed, Feryan, Iyer, Subashree, Lin, Weimin, Walker, Joel, Zhao, He
Format Journal Article
LanguageEnglish
Published OXFORD Elsevier Ltd 23.06.2010
Elsevier
Subjects
Chemistry
Chemistry, Organic
Physical Sciences
Science & Technology
POTENT
PRIVILEGED STRUCTURES
CATALYZED SYNTHESIS
ARYL HALIDES
IMATINIB
INHIBITORS
DISCOVERY
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Summary:A method for the efficient assembly of novel 4-aryl- and 4-anilino-2-(heteroarylamino)pyrimidines via Buchwald–Hartwig N-arylations at elevated temperatures under sealed tube conditions is reported. 4-Aryl-2-anilinopyrimidines and 2,4-dianilinopyrimidines are privileged structures found in many drug-like molecules and biologically active compounds. A method for the quick assembly of novel 4-aryl- and 4-anilino-2-(heteroarylamino)pyrimidines via Buchwald–Hartwig N-arylations at elevated temperatures under sealed tube conditions is reported. This method’s convenience and practicality is demonstrated through the preparation of several novel non-nucleoside reverse transcriptase inhibitor (NNRTI) analogues.
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ISSN:0040-4039
1873-3581
DOI:10.1016/j.tetlet.2010.04.062