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Synthesis of Substituted Aminopyrimidines as Novel Promising Tyrosine Kinase Inhibitors

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Abstract

A procedure has been proposed for the synthesis of a series of substituted N-(1,3-thiazol-2-yl)-pyrimidin-2-amines and N-(pyrimidin-2-yl)thioureas by reactions of diethyl 2-(ethoxymethylidene)malonate and ethyl 2-(ethyoxymethylidene)-3-oxobutanoate with 1,3-thiazol-2-ylguanidines and amidinothiourea, respectively. Preliminary screening has revealed high inhibitory activity of ethyl 2-(carbamothioylamino)-4-methylpyrimidine-5-carboxylate and ethyl 2-(carbamothioylamino)-6-oxo-1,6-dihydropyrimidine-5-carbox-ylate toward several protein kinases.

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Funding

This study was performed under financial support by the Russian Science Foundation (project no. 18-74-10097).

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Correspondence to N. V. Stolpovskaya.

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The authors declare the absence of conflict of interests.

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Russian Text © The Author(s), 2019, published in Zhurnal Organicheskoi Khimii, 2019, Vol. 55, No. 9, pp. 1406–1414.

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Stolpovskaya, N.V., Kruzhilin, A.A., Zorina, A.V. et al. Synthesis of Substituted Aminopyrimidines as Novel Promising Tyrosine Kinase Inhibitors. Russ J Org Chem 55, 1322–1328 (2019). https://doi.org/10.1134/S1070428019090094

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  • DOI: https://doi.org/10.1134/S1070428019090094

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