Kazan medical journalKazan medical journal0368-48142587-9359Eco-Vector10058410.17816/kazmj100584Research ArticleUse of synthetic equivalents of dipolar [C2] 2/2+ -synthons for synthesis of biologically active heterocyclic assemblies with coumarin linksKovalenkoS. N.<p>Department of Organic Chemistry</p>info@eco-vector.comChernykhV. P.<p>Department of Organic Chemistry</p>info@eco-vector.comBelokonYa. V.<p>Department of Organic Chemistry</p>info@eco-vector.comOrlenkoI. V.<p>Department of Organic Chemistry</p>info@eco-vector.comZhuravelI. A.<p>Department of Organic Chemistry</p>info@eco-vector.comNikitchenkoV. M.<p>Department of Organic Chemistry</p>info@eco-vector.comSilinA. V.<p>Department of Organic Chemistry</p>info@eco-vector.comUkrainian Pharmaceutical Academy150519957631891931202202212022022Copyright © 1995, Eco-Vector1995<p>Within the synthon approach the analysis of synthetical potential of the dipolar [C<sub>2</sub>] 2/2<sup>+</sup> - synthons is performed. The possible reaction pathways of cyclization of the dipolar electrophilic <math xmlns="http://www.w3.org/1998/Math/MathML"><msubsup><mrow><mo>[</mo><msub><mi>C</mi><mn>2</mn></msub><mo>]</mo></mrow><mn>2</mn><mrow><mn>2</mn><mo>+</mo></mrow></msubsup></math>-synthons with the dipolar nucleophilic <math xmlns="http://www.w3.org/1998/Math/MathML"><msubsup><mrow><mo>[</mo><mi>S</mi><mi>N</mi><mo>]</mo></mrow><mn>3</mn><mrow><mn>2</mn><mo>-</mo></mrow></msubsup></math>, <math xmlns="http://www.w3.org/1998/Math/MathML"><msubsup><mrow><mo>[</mo><mi>S</mi><mi>N</mi><mo>]</mo></mrow><mn>4</mn><mrow><mn>2</mn><mo>-</mo></mrow></msubsup></math>, <math xmlns="http://www.w3.org/1998/Math/MathML"><msubsup><mrow><mo>[</mo><mi>C</mi><mi>N</mi><mo>]</mo></mrow><mn>3</mn><mrow><mn>2</mn><mo>-</mo></mrow></msubsup></math>, <math xmlns="http://www.w3.org/1998/Math/MathML"><msubsup><mrow><mo>[</mo><msub><mi>N</mi><mn>2</mn></msub><mo>]</mo></mrow><mn>3</mn><mrow><mn>2</mn><mo>-</mo></mrow></msubsup></math>-synthons are determined. As synthetical equivalents of <math xmlns="http://www.w3.org/1998/Math/MathML"><msubsup><mrow><mo>[</mo><msub><mi>C</mi><mn>2</mn></msub><mo>]</mo></mrow><mn>2</mn><mrow><mn>2</mn><mo>+</mo></mrow></msubsup></math>-synthons, 3-(-bromoacetyl) coumarins are chosen. On the basis of the new and improved methods of syntheseis two- and threelink biologically active assemlies of cycles with terminal coumarin links containing thriazole, indolizine, azoindolizine, 1, 3, 4-thiadiazine, furane, quinoxaline and oxazole rings are synthesized. The biological activity of 3-thiazolylcoumarins is investigated. It is stated that all of the compounds under investigation are low toxic and some of them manifest the pronounetd diuretic, antiinflammatory and membrane-stabilizing activities.</p>Kazan Medical archiveКазанский медицинский архив