Synthesis of Novel Benzothiophene Derivatives via Cyclization Reactions

Hama, A. K.; Algso, Muheb A. S.; Kavak, Emrah; Kıvrak, Arif

doi:10.1134/s1070428020070222

Cited by 4 publications

References 25 publications

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Iodocyclization of 2‐Methylthiophenylacetylenes to 3‐Iodobenzothiophenes and their coupling Reactions under More Sustainable Conditions

et al. 2022

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We report the first example of iodocyclization of readily available 2‐methylthiophenylacetylenes in a deep eutectic solvent (ChCl/urea 1/2, mol/mol) as recyclable and more sustainable solvent with respect to the classical VOCs employed so far. The process successfully afforded a variety of 3‐iodobenzothiophenes in good to high yields starting from differently substituted substrates, with the possibility to recycle the DES several times without appreciable lowering of the product yield. The 3‐iodothiophenes thus synthesized are known to be important precursors of biologically active molecules and functionalized heterocycles, and were successfully employed for performing representative Sonogashira and Suzuki cross‐coupling reactions. The solvent‐catalyst system could be conveniently recycled several times without any loss of activity in both coupling processes, thus further demonstrating the practical usefulness of our approach.

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Iodocyclization of 2‐Methylthiophenylacetylenes to 3‐Iodobenzothiophenes and their coupling Reactions under More Sustainable Conditions

et al. 2022

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Synthesis of Ethynyl‐Thiophene Derivatives, Antioxidant Properties and ADME Analysis

et al. 2022

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Herein, novel alkyne based organic compounds, 2‐((2‐(methylthio)phenyl)ethynyl)thiophene (MAT) and 2‐ethynyl‐3‐(phenylethynyl)thiophene (DAT), were designed and synthesized via Pd‐catalyst cross‐coupling reactions. The isolated yields of MAT and DAT were obtained as 77 % and 96 %, respectively. After chemical characterization, radical scavenging activities and reduction power capacities of them were determined by DPPH, TEAC, phosphomolybdenum and reducing power methods. MAT showed higher radical scavenging activities than DAT, and comparable with the standard. Moreover, basic ADME properties were calculated in silico. Both of the newly synthesized derivatives were reported with the same moderate to good drug score of 0.42; and, having potential to pass through BBB and GI with no appointed toxic effects.

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Catalytic electro-oxidation of hydrazine by thymol based-modified glassy carbon electrode

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Kıvrak

Ozok-Arici

et al. 2022

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Synthesis of Novel Benzothiophene Derivatives via Cyclization Reactions

Cited by 4 publications

References 25 publications

Iodocyclization of 2‐Methylthiophenylacetylenes to 3‐Iodobenzothiophenes and their coupling Reactions under More Sustainable Conditions

Iodocyclization of 2‐Methylthiophenylacetylenes to 3‐Iodobenzothiophenes and their coupling Reactions under More Sustainable Conditions

Synthesis of Ethynyl‐Thiophene Derivatives, Antioxidant Properties and ADME Analysis

Catalytic electro-oxidation of hydrazine by thymol based-modified glassy carbon electrode

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