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Synthesis of Pyrimido[2,1-b][1,3,5]Thiadiazines Containing Polyfluoroalkyl- and Amino Acid Fragments

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Chemistry of Heterocyclic Compounds Aims and scope

8-Polyfluoroalkylpyrimido[2,1-b][1,3,5]thiadiazine-6-ones containing a structural fragment of amino acid or its ester were synthesized by a multicomponent cyclization of 6-polyfluoroalkyl-2-thiouracils with formaldehyde and amines. The use of diamino acids allowed the preparation of bis(pyrimido-[2,1-b][1,3,5]thiadiazin-6-ones), containing an aliphatic linker with a carboxy group. Two of the synthesized compounds exhibited weak antituberculosis activity in vitro.

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The work was performed with financial support from the Russian Foundation for Basic Research (grant 13-03-00617), the Program of Ural Branch of the Russian Academy of Sciences (project 12-М-34-2064), and the Grants Council of the President of the Russian Federation (grant NSh-3656.2014.3).

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Correspondence to Ya. V. Burgart.

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Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 6, pp. 976-982, June, 2014.

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Khudina, O.G., Ivanova, A.E., Burgart, Y.V. et al. Synthesis of Pyrimido[2,1-b][1,3,5]Thiadiazines Containing Polyfluoroalkyl- and Amino Acid Fragments. Chem Heterocycl Comp 50, 901–906 (2014). https://doi.org/10.1007/s10593-014-1544-x

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