In this article, we report a regioselective method for the synthesis of new water-soluble 1,3,4-trisubstituted tetrahydropyrimidin-2(1H)-one derivatives containing sodium methanesulfonate fragment in the first position of the heterocycle. The method is based on the reaction of (1-(3,3-diethoxypropyl)ureido)methanesulfonate with aromatic and heterocyclic nucleophiles. The proposed method is distinguished by the possibility of obtaining a wide range of water-soluble substituted tetrahydropyrimidinone derivatives, the absence of the need to use expensive metal complex catalysts, high product yield, and ease of purification.
Keywords: tetrahydropyrimidin-2(1H)-one; electrophilic substitution; C-nucleophiles; acetals
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Smolobochkin, A. V.; Gazizov, A. S.; Yakhshilikova, L. J.; Sidlyaruk, N. A.; Khamatgalimov, A. R.; Burilov, A. R.; Pudovik, M. A. Beilstein Arch. 2022, 202232. doi:10.3762/bxiv.2022.32.v1
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