Microwave-assisted synthesis of 2,5-disubstituted pyrimidine derivatives via Buchwald-Hartwig amination

[Display omitted] •A practical procedure was developed to prepare 2,5-disubstituted pyrimidines.•The method has a wide range of substrate scope and good functional group tolerance.•The reaction occurred generally in good to excellent yields.•The products of this reaction could be used as the buildin...

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Bibliographic Details
Published in:Tetrahedron letters Vol. 61; no. 3; p. 151406
Main Authors: Li, Bo, Etheve-Quelquejeu, Mélanie, Yen-Pon, Expédite, Garbay, Christiane, Chen, Huixiong
Format: Journal Article
Language:English
Published: Elsevier Ltd 16-01-2020
Elsevier
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Summary:[Display omitted] •A practical procedure was developed to prepare 2,5-disubstituted pyrimidines.•The method has a wide range of substrate scope and good functional group tolerance.•The reaction occurred generally in good to excellent yields.•The products of this reaction could be used as the building blocks in drug design. Various 2,5-disubstituted pyrimidine derivatives were synthesized under microwave irradiation via Buchwald-Hartwig amination. This concise approach provides interesting scaffolds in good to high yields and with large functional group compatibility. These novel chemical entities could be used as building blocks in drug design.
ISSN:0040-4039
1873-3581
DOI:10.1016/j.tetlet.2019.151406