Pyrimidines are the key skeletons in numerous bioactive compounds and natural products[1]. A pyrimidine has many properties, electrophilic aromatic substitution gets more difficult while nucleophilic aromatic substitution gets easier[2]. In particular, a variety of pyrimidine-derived drugs have demonstrated interesting biological activities such as cyclin-dependent kinases (CDK), tumor necrosis factor α (TNF-α), ableson protein tyrosine kinase (Abl), 3-phosphatidylinositol kinases (PI-3K), protein kinase B (Akt kinase), cytokines inhibitors[1, 3] and so on[4-7]. Over a century, pyrimidine derivatives are important azaheterocycles that have inspired the development of new methodologies for their chemical synthesis[2].
[1] Organic Letters (2020), 22(14), 5645-5649.
[2] Journal of Heterocyclic Chemistry (2020), Ahead of Print. DOI: 10.1002/jhet.4070.
[3] Journal of Medicinal Chemistry (2011), 54(9), 3200-3205.
[4] Journal of Medicinal Chemistry (2016), 59(15), 7268-7274.
[5] Journal of Medicinal Chemistry (2020), Ahead of Print. DOI:
[6] Journal of Medicinal Chemistry (2019), 62(22), 10376-10390.
[7] European Journal of Medicinal Chemistry (2019), 163, 169-182.
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