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

• 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
• Subjects: C[sbnd]N cross-coupling; Chemical Sciences; Microwave synthesis; Pd-catalyzed; Pyrimidine; CN cross-coupling; Microwave synthesis; Pd-catalyzed; Pyrimidine
• ISSN: 0040-4039; 1873-3581
• DOI: 10.1016/j.tetlet.2019.151406

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•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.