Concise, flexible syntheses of 4-(4-imidazolyl) pyrimidine cyclin-dependent kinase 2 (CDK2) inhibitors

M Toumi, M Barbazanges, SHB Kroll, H Patel, S Ali…

文献索引：Toumi, Mathieu; Barbazanges, Marion; Kroll, Sebastian H.B.; Patel, Hetal; Ali, Simak; Coombes, R. Charles; Barrett, Anthony G.M. Tetrahedron Letters, 2010 , vol. 51, # 47 p. 6126 - 6128

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被引用次数: 1

摘要

A flexible six-step synthesis of potential cyclin-dependent kinase 2 (CDK2) inhibitors is reported. The synthesis involves the condensation between 3-chloro-4, 4-dimethoxy-2- butanone and amidines, which provides acetyl-imidazoles and late stage palladium- catalyzed N-arylation to give the target pyrimidine derivatives.

~6%

Imidazoles: SAR and development of a potent class of cyclin-...

[Anderson, Malcolm; Andrews, David M.; Barker, Andy J.; Brassington, Claire A.; Breed, Jason; Byth, Kate F.; Culshaw, Janet D.; Finlay, M. Raymond V.; Fisher, Eric; McMiken, Helen H.J.; Green, Clive P.; Heaton, Dave W.; Nash, Ian A.; Newcombe, Nicholas J.; Oakes, Sandra E.; Pauptit, Richard A.; Roberts, Andrew; Stanway, Judith J.; Thomas, Andrew P.; Tucker, Julie A.; Walker, Mike; Weir, Hazel M. Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 20 p. 5487 - 5492]