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Journal articles on the topic 'Synthesis of Thioureas'

Author: Grafiati

Published: 5 June 2025

Last updated: 1 August 2025

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1

Ngaini, Zainab, Wan Sharifatun Handayani Wan Zulkiplee, and Ainaa Nadiah Abd Halim. "One-Pot Multicomponent Synthesis of Thiourea Derivatives in Cyclotriphosphazenes Moieties." Journal of Chemistry 2017 (2017): 1–7. http://dx.doi.org/10.1155/2017/1509129.

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In this study, hexasubstituted thiourea was carried out via reaction of isothiocyanato cyclophosphazene intermediates with a series of aromatics amines and amino acids in a one-pot reaction system. The reaction was not as straightforward as typical thiourea synthesis. Six unexpected thiourea derivatives3a–fwere formed in the presence of cyclotriphosphazene moieties in good yields (53–82%). The structures of3a–fwere characterized by elemental analysis and FTIR,1H,13C, and31P NMR spectroscopies. The occurrence of reverse thioureas formation in a one-pot reaction system is discussed. The possible

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2

Milosavljevic, Milutin, Ivan Vukicevic, Veis Serifi, et al. "Optimization of the synthesis of N-alkyl and N,N-dialkyl thioureas from waste water containing ammonium thiocyanate." Chemical Industry and Chemical Engineering Quarterly 21, no. 4 (2015): 501–10. http://dx.doi.org/10.2298/ciceq141221006m.

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The optimized methods for N-alkyl and N,N-dialkyl substituted thioureas synthesis starting from ammonium thiocyanates, waste water constituent from the production of tetramethylthiuram monosulfide (TMTS), and alkyl amine, are presented in this work. Therefore, thioureas synthesis was developed in two ways: Method I - reaction of the thiocyanate and alkylamine in the presence of hydrochloric acid; Method II - reaction of the thiocyanate with benzoyl chloride following by amine addition in the first step, and base hydrolysis in the second step. The structure of the synthesized compounds was conf

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3

Siddharth A. Waghmare and Swapnil B. Sarkate. "Design, synthesis and characterization of some novel Thiocarbamidopyrimidines." International Journal of Science and Research Archive 10, no. 2 (2023): 895–99. http://dx.doi.org/10.30574/ijsra.2023.10.2.1034.

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Interaction of 2 chloro pyrimidines with various substituted thioureas such as thiourea, N- phenylthiourea, 1,3 Dimethylthiourea, N- allylthiourea and ethyl thiourea were carried in presence of isopropanol as a medium. The product isolated in these reactions were characterized on the basis of elemental analysis, chemical characteristics and spectral studies.

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4

Elshaier, Yaseen A. M. M., Ashraf A. Aly, Mohamed Abdel-Aziz, et al. "Synthesis and Identification of New N,N-Disubstituted Thiourea, and Thiazolidinone Scaffolds Based on Quinolone Moiety as Urease Inhibitor." Molecules 27, no. 20 (2022): 7126. http://dx.doi.org/10.3390/molecules27207126.

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Synthesis of thiazolidinone based on quinolone moiety was established starting from 4-hydroxyquinol-2-ones. The strategy started with the reaction of ethyl bromoacetate with 4-hydroxyquinoline to give the corresponding ethyl oxoquinolinyl acetates, which reacted with hydrazine hydrate to afford the hydrazide derivatives. Subsequently, hydrazides reacted with isothiocyanate derivatives to give the corresponding N,N-disubstituted thioureas. Finally, on subjecting the N,N-disubstituted thioureas with dialkyl acetylenedicarboxylates, cyclization occurred, and thiazolidinone derivatives were obtain

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5

Erol Günal, Şule, and Engin Kaplan. "SYNTHESIS, EVALUATION OF ANTIFUNGAL ACTIVITY AND DRUG-LIKENESS OF BENZOYL THIOUREA DERIVATIVES." İstanbul Ticaret Üniversitesi Fen Bilimleri Dergisi 24, no. 47 (2025): 217–28. https://doi.org/10.55071/ticaretfbd.1588118.

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Herein, we report the synthesis of a series of 2-bromobenzoyl-substituted thiourea derivatives. The structures of the synthesized thioureas were characterized by spectroscopic methods. These derivatives, together with 2-fluorobenzoyl thioureas synthesized previously, have been evaluated for their potential antifungal activity. Compounds 2d and 2f showed antifungal activity against Candida albicans. Compound 2f also demonstrated activity against C. parapsilosis. Drug-likeness properties of the compounds were also estimated, and it was found that all compounds showed good drug-likeness propertie

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6

Chrzanowski, Jacek, Luca Sancineto, Malgorzata Deska, Michal Rachwalski, and Jozef Drabowicz. "Thioureas Derived from (S)-1-(2-pyridyl)ethylamine Enantiomer: Synthesis and Selected Applications as an Organocatalyst." Symmetry 17, no. 2 (2025): 216. https://doi.org/10.3390/sym17020216.

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In order to expand the group of chiral thiourea structures, several optically active thioureas derived from the (S)-1-(2-pyridyl)ethylamine enantiomer were prepared via its reaction with achiral or optically active isothiocyanates. To show their synthetic potential as chiral auxiliaries the isolated thioureas were tested as an optically active organocatalyst in the asymmetric version of the selected aldol condensation and addition of diethylzinc to benzaldehyde. The observation of asymmetric induction in these model reactions encourages further research on the use of this group of thioureas in

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7

Chayah, Mariem, M. Encarnación Camacho, M. Dora Carrión, Miguel A. Gallo, Miguel Romero, and Juan Duarte. "N,N′-Disubstituted thiourea and urea derivatives: design, synthesis, docking studies and biological evaluation against nitric oxide synthase." MedChemComm 7, no. 4 (2016): 667–78. http://dx.doi.org/10.1039/c5md00477b.

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8

Mojtahedi, Mohammad M., Mohammad R. Saidi, and Mohammad Bolourtchian. "A Novel Method for the Synthesis of Disubstituted Ureas and Thioureas under Microwave Irradiaton." Journal of Chemical Research 23, no. 12 (1999): 710–11. http://dx.doi.org/10.1177/174751989902301213.

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Several symmetrically disubstituted ureas and thioureas are synthesized by heating of urea or thiourea with aromatic amines or phenylhydrazine under environmentally benign conditions without any solvent in a conventional microwave oven.

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9

Dhaene, Evert, Isabel Van Driessche, Klaartje De Buysser, and Kristof Van Hecke. "Crystal structures of three N,N,N′-trisubstituted thioureas for reactivity-controlled nanocrystal synthesis." Acta Crystallographica Section E Crystallographic Communications 78, no. 2 (2022): 184–90. http://dx.doi.org/10.1107/s2056989022000147.

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The synthesis and single-crystal X-ray structures of three N,N,N′-trisubstituted thioureas are reported, namely N,N,N′-tribenzylthiourea, C22H22N2S (1), N-methyl-N,N′-diphenylthiourea, C14H14N2S (2), and N,N-di-n-butyl-N′-phenylthiourea, C15H24N2S (3). The influence of the different substituents on the thioureas is clear from the delocalization of the thiourea C—N and C=S bonds, while the crystal structures show infinite chains of N,N,N′-tribenzylthiourea (1), hydrogen-bonded pairs of N-methyl-N,N′-diphenylthiourea (2) and hexamer ring assemblies of N,N-di-n-butyl-N′-phenylthiourea (3) molecul

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10

Al-Riyahee, Ali A. A. "First Row Transition Metal Complexes Derived from N, Nʹ-Substituted Thiourea: Synthesis, Geometrical Structures and Cyclic Voltammetry Probe: A Review". BASRA JOURNAL OF SCIENCE 39, № 1 (2021): 96–118. http://dx.doi.org/10.29072/basjs.202117.

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Thioureas or thiourea derivatives as organosulfur compounds are one of the most widely used ligands in different applications as we are going to discuss it extensively such as in coordination chemistry by involving them to rich sources of N, O and S atoms coordinating through S atom, S and O atoms in benzoyl derivatives or S, O and N atoms in pyridyl hetrocylic benzoyl derivatives. These hard and soft donor sites facilitate the bonding between thiourea free ligand and metal ion through one or more to make ligands behave as mono, bi or multidentate ligands to form huge and stable series of the

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11

Journal, Baghdad Science. "Synthesis of New Amide and ThioUrease Compounds." Baghdad Science Journal 4, no. 3 (2007): 430–37. http://dx.doi.org/10.21123/bsj.4.3.430-437.

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The reaction of some new Schiff bases ( 2-[(2-Amino – ethylimino)-methyl]-R , 2-({2-[(R-benzylidene)-amino]-ethylimino}-methyl)-R with Benzoyl chloride or Acetyl chloride were carried out. Subsequent reactions of these products N-(2-Amino-ethyl)-N-[Chloro-(R) –methyl]-benzamide or N-(2-{?-[chloro-(R) –methyl]-amino}-ethyl)-N-[chloro-(R) –methyl]- benzamide with thiourea afforded thioureas compounds. The synthesized compounds were confirmed by their IR,UV,spectra and C.H.N. analysis.

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12

Milosavljevic, Milutin, Ivan Vukicevic, Sasa Drmanic, et al. "Simple one-pot synthesis of thioureas from amine, carbon disulfide and oxidants in water." Journal of the Serbian Chemical Society 81, no. 3 (2016): 219–31. http://dx.doi.org/10.2298/jsc150831087m.

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The present study reports the new facile methodology for synthesis of symmetrical and asymmetrical thioureas by an one-pot reaction of amine, carbon disulfide and oxidants: hydrogen peroxide, ethylenediamine tetraacetic acid (EDTA)/sodium percarbonate system or air. The structures of the synthesized compounds were confirmed by IR, 1H and 13C NMR and MS methods. Reaction mechanism has been proposed on the basis of reaction intermediate isolation and their structure determination. The synthetic benefits of the presented methods is reflected in the operational simplicity, mild reaction conditions

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13

Mahadevaiah, Raghavendra, Lalithamba Haraluru Shankraiah та Latha Haraluru Kamalamma Eshwaraiah. "Combustion Synthesis of Nano Fe2O3 and its Utilization as a Catalyst for the Synthesis of Nα-Protected Acyl Thioureas and Study of Anti-bacterial Activities". Acta Chimica Slovenica 69, № 1 (2022): 116–24. https://doi.org/10.17344/acsi.2021.7055.

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A simple and eco-friendly nano Fe2O3 heterogeneous catalytic system is described for the synthesis of acyl thiourea derivatives from corresponding in situ generated acyl isothiocyanates and amino acid esters in acetone obtained in good yields. The structures of synthesized acyl thioureas were confimed by 1H NMR, 13C NMR, mass, and FTIR analysis. Fe2O3 NPs has been prepared via a solution combustion route using ascorbic acid as the reducing agent and ferric nitrate as the source of iron. The prepared nano material has been characterized by XRD, SEM, UV-Visible, and FTIR analysis. More prominent

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14

Qureshi, Farah, Muhammad Yar Khuhawar, Taj Muhammad Jahangir, and Abdul Hamid Channar. "Synthesis and Characterization of Multicolor Luminescent and Thermally Stable Thioureas and Polythioamides." Acta Chimica Slovenica 70, no. 4 (2023): 560–73. http://dx.doi.org/10.17344/acsi.2022.7668.

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Two new polythioamides were prepared through the polycondensation reaction between thiourea monomers and terephthaloyl dichloride, while the thiourea monomers were synthesized by the interaction of aromatic (4,4’-diaminophenylsulfone) or alicyclic (1,2-cyclohexanediamine) diamine with ammonium thiocyanate. The elemental composition of polythioamides was confirmed through CHN microanalysis. The structure and properties of thiourea monomers and polythioamides were determined through proton NMR, UV-Vis, FT-IR spectroscopy, fluorescence, TGA/DTA and SEM. The polythioamides indicated high thermal s

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15

Todorova, Stanislava E., Rusi I. Rusew, Zhanina S. Petkova, Boris L. Shivachev, and Vanya B. Kurteva. "Novel Thiourea Ligands—Synthesis, Characterization and Preliminary Study on Their Coordination Abilities." Molecules 29, no. 20 (2024): 4906. http://dx.doi.org/10.3390/molecules29204906.

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Two series of polydentate N,O,S-ligands containing thiourea fragments attached to a p-cresol scaffold, unsymmetrical mono-acylated bis-amines and symmetrical bis-thioureas, are obtained by common experiments. It is observed that the reaction output is strongly dependent on both bis-amine and thiocarbamic chloride substituents. The products are characterized by 1D and 2D NMR spectra in solution and by single crystal XRD. A preliminary study on the coordination abilities of selected products is performed by ITC at around neutral media.

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16

Steppeler, Franz, Dominika Iwan, Elżbieta Wojaczyńska, and Jacek Wojaczyński. "Chiral Thioureas—Preparation and Significance in Asymmetric Synthesis and Medicinal Chemistry." Molecules 25, no. 2 (2020): 401. http://dx.doi.org/10.3390/molecules25020401.

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For almost 20 years, thioureas have been experiencing a renaissance of interest with the emerged development of asymmetric organocatalysts. Due to their relatively high acidity and strong hydrogen bond donor capability, they differ significantly from ureas and offer, appropriately modified, great potential as organocatalysts, chelators, drug candidates, etc. The review focuses on the family of chiral thioureas, presenting an overview of the current state of knowledge on their synthesis and selected applications in stereoselective synthesis and drug development.

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17

Koutoulogenis, Giorgos, Nikolaos Kaplaneris, and Christoforos G. Kokotos. "(Thio)urea-mediated synthesis of functionalized six-membered rings with multiple chiral centers." Beilstein Journal of Organic Chemistry 12 (March 10, 2016): 462–95. http://dx.doi.org/10.3762/bjoc.12.48.

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Organocatalysis, now running its second decade of life, is being considered one of the main tools a synthetic chemist has to perform asymmetric catalysis. In this review the synthesis of six-membered rings, that contain multiple chiral centers, either by a ring closing process or by a functionalization reaction on an already existing six-membered ring, utilizing bifunctional (thio)ureas will be summarized. Initially, the use of primary amine-thioureas as organocatalysts for the above transformation is being discussed, followed by the examples employing secondary amine-thioureas. Finally, the u

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18

Poláčková, Viera, Dominika Krištofíková, Boglárka Némethová, Renáta Górová, Mária Mečiarová, and Radovan Šebesta. "N-Sulfinylpyrrolidine-containing ureas and thioureas as bifunctional organocatalysts." Beilstein Journal of Organic Chemistry 17 (October 25, 2021): 2629–41. https://doi.org/10.3762/bjoc.17.176.

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The synthesis of bifunctional <em>N</em>-sulfinylureas and thioureas with an appended pyrrolidine unit is presented. These organocatalysts were evaluated in Michael additions of aldehydes to nitroalkenes both under solvent-free conditions and in solution. The <em>N</em>-sulfinylurea catalyst was more efficient than the corresponding thiourea. For some substrates, enantioselectivities reached 98% ee. The stereogenic center on the sulfur did not have a considerable influence on the catalytic reactions. Under ball-milling conditions, the Michael adducts were obtained in good yields but with sligh

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19

Kovalskaya, A. V., A. N. Lobov, V. V. Zarubaev, and I. P. Tsypysheva. "Derivatives of (–)-Cytisine with Thiourea Fragment. Synthesis and Antiviral Activity." Žurnal obŝej himii 94, no. 6 (2024): 712–21. http://dx.doi.org/10.31857/s0044460x24060054.

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New derivatives of the quinolizidine alkaloid, (–)-cytisine, with a substituted 2-pyridone ring and a thiourea moiety in the bispidin fragment of the molecule were synthesized. The ability of the synthesized cytisine-containing thioureas to inhibit the reproduction of human parainfluenza virus type 3 was assessed. It was found that the derivatives obtained by the reaction of benzoyl or phenyl isothiocyanate with (–)-cytisine, as well as its 9-bromo or 9,11-derivative, effectively suppress the reproduction of human parainfluenza virus type 3 (their selectivity indices are 56, 58 and 95, respect

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20

V., Madhura, Hrishikesh M. Revankar, and Manohar V. Kulkarni. "A new route for the synthesis of 4-arylacetamido-2-aminothiazoles and their biological evaluation." Zeitschrift für Naturforschung B 70, no. 7 (2015): 483–89. http://dx.doi.org/10.1515/znb-2015-0013.

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AbstractA series of 4-arylacetamido-2-amino- and 2-arylamino-1,3-thiazoles (4a–o) were synthesized in a single step in high yields from ω-bromoacetoacetanilides and thiourea/phenyl thioureas and were characterized by spectral and analytical methods. The compounds were evaluated for their in vitro antibacterial antifungal and antioxidant activities. In vitro antimicrobial evaluation of these compounds indicated their specificity towards Gram-positive species. p-Tolyl and m-chlorophenyl substituents on the arylamino moiety (compounds 4b and 4g) exhibited the lowest minimum inhibitory concentrati

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21

Habila, Tahir, Mebrouk Belghobsi, Mohamed-Zakaria Stiti, et al. "Synthesis and vasodilator activity of 3,4-dihydropyrimidin-2(1H)-ones bearing urea, thiourea, and sulfonylurea moieties." Canadian Journal of Chemistry 97, no. 1 (2019): 20–28. http://dx.doi.org/10.1139/cjc-2018-0239.

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A series of novel 3,4-dihydropyrimidin-2(1H)-ones bearing urea, thiourea, and sulfonylurea moieties were synthesized and pharmacologically evaluated as vasodilator agents. The most interesting vasodilators were the thiourea derivatives 6a and 6b and the urea derivatives 6f–6i and 7f–7h, although the ureas were relatively more active than thioureas. Twenty-fold more active than diazoxide, the urea 6g was the most potent vasodilator (EC50 = 0.983 ± 0.061 μmol/L) and proved to act as a voltage-gated calcium channel blocker. The lack of activity of sulfonylureas, 6k and 7j, could be attributed to

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22

Singh, Gurdial, Pooja Sharma, Bhoomendra A. Bhongade, Malleshappa N. Noolvi, and Andanappa K. Gadad. "Synthesis of 5-Fluoroaminobenzothiazoles." SynOpen 04, no. 02 (2020): 23–32. http://dx.doi.org/10.1055/s-0040-1707105.

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A series of 5-fluoro-2-(N-substituted)aminobenzothiazoles were synthesized by intramolecular cyclisation of the corresponding thioureas, which were prepared by treatment of 4-substituted 3-fluoroanilines with appropriate isothiocyanates.

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23

Valle, María, Laura Martín, Alicia Maestro, José M. Andrés, and Rafael Pedrosa. "Chiral Bifunctional Thioureas and Squaramides Grafted into Old Polymers of Intrinsic Microporosity for Novel Applications." Polymers 11, no. 1 (2018): 13. http://dx.doi.org/10.3390/polym11010013.

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We have prepared different polymeric chiral bifunctional thioureas and squaramides by modification of the very well-known polymers of intrinsic microporosity (PIM), specifically PIM-1 and PIM-CO-1, to be used as recoverable organocatalysts. The installation of the chiral structures into the polymers has been done in two or three steps in high yields. The catalytic activity of the resulting materials has been proved in the stereoselective nitro-Michael addition and in a cascade process, which allows the synthesis of enantioenriched 4H-chromene derivatives. Squaramide II and thiourea III have be

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24

Thanh, Nguyen Dinh. "Synthesis of Peracetylatedβ-D-Glucopyranosyl Thioureas from Substituted 2-Aminobenzo-1ʹ, 3ʹ-thiazoles". E-Journal of Chemistry 9, № 1 (2012): 55–62. http://dx.doi.org/10.1155/2012/615601.

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Some peracetylated glucopyranosyl thioureas containing a heterocyclic ring system, benzo-1,3-thiazole have been prepared by the condensation reaction of tetra-O-acetyl-β-D-glucopyranosyl isothiocyanate and corresponding substituted 2-amino-(6-substituted)benzo-1,3-thiazoles. Investigated heating conditions showed that the solventless microwave-assisted method gave higher yields of these thioureas.

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25

Ketz, Hartmut, Werner Tjarks, and Detlef Gabel. "Synthesis of nido-carborate containing thioureas." Tetrahedron Letters 31, no. 28 (1990): 4003–6. http://dx.doi.org/10.1016/s0040-4039(00)94483-6.

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26

Németh, András Gy, Renáta Szabó, György Orsy, István M. Mándity, György M. Keserű, and Péter Ábrányi-Balogh. "Continuous-Flow Synthesis of Thioureas, Enabled by Aqueous Polysulfide Solution." Molecules 26, no. 2 (2021): 303. http://dx.doi.org/10.3390/molecules26020303.

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We have developed the continuous-flow synthesis of thioureas in a multicomponent reaction starting from isocyanides, amidines, or amines and sulfur. The aqueous polysulfide solution enabled the application of sulfur under homogeneous and mild conditions. The crystallized products were isolated by simple filtration after the removal of the co-solvent, and the sulfur retained in the mother liquid. Presenting a wide range of thioureas synthesized by this procedure confirms the utility of the convenient continuous-flow application of sulfur.

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27

Németh, András Gy, Renáta Szabó, György Orsy, István M. Mándity, György M. Keserű, and Péter Ábrányi-Balogh. "Continuous-Flow Synthesis of Thioureas, Enabled by Aqueous Polysulfide Solution." Molecules 26, no. 2 (2021): 303. http://dx.doi.org/10.3390/molecules26020303.

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We have developed the continuous-flow synthesis of thioureas in a multicomponent reaction starting from isocyanides, amidines, or amines and sulfur. The aqueous polysulfide solution enabled the application of sulfur under homogeneous and mild conditions. The crystallized products were isolated by simple filtration after the removal of the co-solvent, and the sulfur retained in the mother liquid. Presenting a wide range of thioureas synthesized by this procedure confirms the utility of the convenient continuous-flow application of sulfur.

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28

Makhsumov, Abduhamid, Yusubjon Holboyev, Nailya Valeeva, Boburbek Ismailov, and Ibragim Askarov. "Synthesis of 1-nicotinoylo-3-(meta-nitrophenyl)- thiourea derivatives with anti-inflammatory activity." E3S Web of Conferences 434 (2023): 02032. http://dx.doi.org/10.1051/e3sconf/202343402032.

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Thiourea derivatives are used in many industries: medicine, agriculture, engineering, rubber industry, organic synthesis. On their basis, various preparations for the needs of the national economy were obtained. The latest studies of thiourea derivatives, carried out at the present time, are prompted not only by theoretical, but also by practical needs. From this point of view, thiourea derivatives are of undoubted interest in substances with different biological activities. They are widely used in agriculture and have been used as herbicides, fungicides, insecticides, bactericides, dyes, grow

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29

Wan, Jie-Ping, Yunfang Lin, Kaikai Hu, and Yunyun Liu. "Secondary amine-initiated three-component synthesis of 3,4-dihydropyrimidinones and thiones involving alkynes, aldehydes and thiourea/urea." Beilstein Journal of Organic Chemistry 10 (January 29, 2014): 287–92. http://dx.doi.org/10.3762/bjoc.10.25.

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The three-component reactions of aldehydes, electron deficient alkynes and ureas/thioureas have been smoothly performed to yield a class of unprecedented 3,4-dihydropyrimidinones and thiones (DHPMs). The reactions are initiated by the key transformation of an enamine-type activation involving the addition of a secondary amine to an alkyne, which enables the subsequent incorporation of aldehydes and ureas/thioureas. This protocol tolerates a broad range of aryl- or alkylaldehydes, N-substituted and unsubstituted ureas/thioureas and alkynes to yield the corresponding DHPMs with specific regiosel

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30

Hurst, DT, AD Stacey, M. Nethercleft, A. Rahim, and MR Harnden. "The Synthesis of Some Pyrimidinyl and Thiazolyl Ureas and Thioureas and Some Related Compounds." Australian Journal of Chemistry 41, no. 8 (1988): 1221. http://dx.doi.org/10.1071/ch9881221.

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Some pyrimidin-2- and pyrimidin-4-amines were treated with isocyanates and isothiocyanates to give the corresponding disubstituted ureas or thioureas . A pyrimidin-2-amine is more reactive than a pyrimidin-4- amine in these reactions. 2-Aminothiazoles and thiazolinones also react to give the disubstituted ureas or thioureas . The use of ethoxycarbonyl or benzoyl isothiocyanate or isocyanate gives products which are readily hydrolysed to the pyrimidinyl or thiazolyureas or thioureas but with concomitant hydrolysis and decarboxylation of an ethoxycarbonyl substituent . The use of chlorosulfonyl

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31

Poláčková, Viera, Dominika Krištofíková, Boglárka Némethová, Renata Górová, Mária Mečiarová, and Radovan Šebesta. "N-Sulfinylpyrrolidine-containing ureas and thioureas as bifunctional organocatalysts." Beilstein Journal of Organic Chemistry 17 (October 25, 2021): 2629–41. http://dx.doi.org/10.3762/bjoc.17.176.

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The synthesis of bifunctional N-sulfinylureas and thioureas with an appended pyrrolidine unit is presented. These organocatalysts were evaluated in Michael additions of aldehydes to nitroalkenes both under solvent-free conditions and in solution. The N-sulfinylurea catalyst was more efficient than the corresponding thiourea. For some substrates, enantioselectivities reached 98% ee. The stereogenic center on the sulfur did not have a considerable influence on the catalytic reactions. Under ball-milling conditions, the Michael adducts were obtained in good yields but with slightly lower enantiom

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32

Viana, Gil Mendes, Edézio Ferreira da Cunha-Junior, Paloma Wetler Meireles Carreiros Assumpção, et al. "Synthesis and Structure–Activity Relationship of Thiourea Derivatives Against Leishmania amazonensis." Pharmaceuticals 17, no. 12 (2024): 1573. http://dx.doi.org/10.3390/ph17121573.

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Background: Leishmaniasis, caused by Leishmania protozoa and transmitted by vectors, presents varied clinical manifestations based on parasite species and host immunity. The lack of effective vaccines or treatments has prompted research into new therapies, including thiourea derivatives, which have demonstrated antiprotozoal activities. Methods: We synthesized two series of N,N′-disubstituted thiourea derivatives through the reaction of isothiocyanates with amines. These compounds were evaluated in vitro against promastigote and amastigote forms of L. amazonensis, alongside cytotoxicity assess

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33

Janovec, Ladislav, Stanislav Böhm, Ivan Danihel, Ján Imrich, Pavol Kristian, and Karel D. Klika. "Theoretical Confirmation of the Reaction Mechanism Leading to Regioselective Formation of Thiazolidin-4-one from Bromoacetic Acid Derivatives." Collection of Czechoslovak Chemical Communications 72, no. 10 (2007): 1435–45. http://dx.doi.org/10.1135/cccc20071435.

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A regioselective synthesis of 3-alkyl-2-[(anthracen-9-yl)imino]thiazolidin-4-ones 2a-2e and 2-(alkylimino)-3-(anthracen-9-yl)thiazolidin-4-ones 3a-3e from appropriate thioureas using methyl bromoacetate or bromoacetyl bromide, respectively, has been rationalized by DFT calculations of model thiourea and its phenyl derivative. The proposed mechanism indicates that the regioselective formation of the target thiazolidinones is a consequence of a different reactivity of the reagents and a varying stability of the intermediates, 1-alkyl-3-(anthracen-9-yl)-2-[(methoxycarbonyl)methyl]isothioureas 4a-

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34

Samakbaeva, M. A., M. G. Babashkina, A. Yu Isaev, and D. A. Safin. "Synthesis and characterization of tetraphenylphosphonium salts of N-phosphorylated thioureas and bis-thioureas." Russian Chemical Bulletin 67, no. 9 (2018): 1738–41. http://dx.doi.org/10.1007/s11172-018-2284-3.

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35

Nurkenov, O. A., S. D. Fazylov, T. M. Seilkhanov, Zh Nurmaganbetov, A. M. Gazaliev, and G. Zh Karipova. "Synthesis and structure of thiourea derivatives of functionally substituted pyridines." Bulletin of the Karaganda University. "Chemistry" series 101, no. 1 (2021): 4–11. http://dx.doi.org/10.31489/2021ch1/4-11.

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The article presents data on the synthesis and study of the structure of thiourea derivatives of functionally substituted pyridines. New thiourea derivatives containing a pharmacologically active pyridine moiety in their structure were obtained. As the starting synton, 2-amino-5-bromopyridine, 2-amino-3-hydroxypyridine and 2-aminomethylpyridine were selected. It was shown that the interaction of 2-amino-5-bromopyridine, 2-amino-3-hydroxypyridine and 2-aminomethylpyridine with ethyl and phenylisothiocyanates in ethanol leads to the formation of the corresponding pyridine-containing thioureas. T

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36

Povidaichyk, M., and M. Onysko. "EFFECTIVE SYNTHESIS OF 5-IODOMETHYL-2-PHENYLIMINOTHIAZOLIDINE." Scientific Bulletin of the Uzhhorod University. Series «Chemistry» 46, no. 2 (2022): 63–67. http://dx.doi.org/10.24144/2414-0260.2021.2.63-67.

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Thioamides and thioureas are interesting building blocks for the synthesis of azaheterocycles with valuable biological properties. The electrophilic cyclization of N-alkenylthioamides and N-alkenylthioureas is one of the methods of their synthesis. It is known that halogen-induced cyclization of N-alkenylthioamides and thioureas leads to the annealing of 5- or 6-membered cycles. In particular, the cyclization of allylthioamides in the presence of halogen gives halomomethylthiazolines. N-allyl-N-arylthioureas react with halogens, arylselenyl chloride or aryl tert-trichloride to form thiazolidin

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37

Lin, Gui-Shan, Chang-Hua Ma, Wen-Gui Duan, Bo Cen, Fu-Hou Lei та Zhang-Qi Yang. "Synthesis and biological activities of α-pinene-based dithiadiazoles". Holzforschung 68, № 1 (2014): 75–83. http://dx.doi.org/10.1515/hf-2013-0006.

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Abstract This work is aiming at the preparation of new bioactive compounds from α-pinene as starting material. To this purpose, the intermediates (disubstituted phenyl acylamino thioureas, class G) were cyclized to dithiadiazoles (class H). The intermediates and target compounds were analyzed by Fourier transform infrared, 1H nuclear magnetic resonance (NMR), 13C NMR, and electrospray ionization-mass spectrometry and elemental analysis. The bioassay experiments showed that the compounds G and H have herbicidal, fungicidal, and plant growth-regulating activities. The compounds 2,2′-dimethylphen

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38

Štrukil, Vjekoslav. "Mechanochemical synthesis of thioureas, ureas and guanidines." Beilstein Journal of Organic Chemistry 13 (September 1, 2017): 1828–49. http://dx.doi.org/10.3762/bjoc.13.178.

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In this review, the recent progress in the synthesis of ureas, thioureas and guanidines by solid-state mechanochemical ball milling is highlighted. While the literature is abundant on their preparation in conventional solution environment, it was not until the advent of solvent-free manual grinding using a mortar and pestle and automated ball milling that new synthetic opportunities have opened. The mechanochemical approach not only has enabled the quantitative synthesis of (thio)ureas and guanidines without using bulk solvents and the generation of byproducts, but it has also been established

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39

Ramadas, K., N. Janarthanan, and S. Velmathi. "Lac Sulfur Assisted Synthesis of Symmetrical Thioureas." Synthetic Communications 27, no. 13 (1997): 2255–60. http://dx.doi.org/10.1080/00397919708003379.

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40

Halimehjani, Azim Ziyaei, and Fataneh Farahbakhsh. "Synthesis of thioureas in ionic liquid medium." Journal of Sulfur Chemistry 34, no. 3 (2012): 284–88. http://dx.doi.org/10.1080/17415993.2012.739623.

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41

KUBOTA, SEIJU, KISAKO HORIE, HEMANTK MISRA, et al. "Synthesis and uncoupling activities of hydrophobic thioureas." CHEMICAL & PHARMACEUTICAL BULLETIN 33, no. 2 (1985): 662–66. http://dx.doi.org/10.1248/cpb.33.662.

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42

Uriel, Clara. "Synthesis of 2-Deoxyglycopyranosyl Thioureas from Glycals." Synthesis 1999, no. 12 (1999): 2049–52. http://dx.doi.org/10.1055/s-1999-3632.

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43

Atwal, Karnail S., Syed Z. Ahmed, and Brian C. O'Reilly. "A facile synthesis of cyanoguanidines from thioureas." Tetrahedron Letters 30, no. 52 (1989): 7313–16. http://dx.doi.org/10.1016/s0040-4039(00)70685-x.

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44

Maryanoff, Cynthia A., Robin C. Stanzione, James N. Plampin, and John E. Mills. "A convenient synthesis of guanidines from thioureas." Journal of Organic Chemistry 51, no. 10 (1986): 1882–84. http://dx.doi.org/10.1021/jo00360a040.

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45

Astashkina, N. V., M. G. Abramyants, D. I. Matveeva, and N. N. Smolyar*. "Synthesis of 4-Aryl(Hetaryl)Spinaceamine Thioureas." Pharmaceutical Chemistry Journal 48, no. 2 (2014): 89–92. http://dx.doi.org/10.1007/s11094-014-1054-2.

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46

Ciszewski, Lech, Daquiang Xu, Oljan Repič, and Thomas J. Blacklock. "Reductive alkylation of thioureas: a highly practical synthesis of unsymmetrical N,N′-disubstituted thioureas." Tetrahedron Letters 45, no. 43 (2004): 8091–93. http://dx.doi.org/10.1016/j.tetlet.2004.08.182.

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47

Mahesh, Kumar Gupta, N. Pandeya Suerendra, M. Zaiad Golal, and S. Gangwar V. "Synthesis and anticonvulsant activity of halo-substituted aryl urea and thioureas." Journal of India Chemical Society Vol. 87, Nov 2010 (2010): 1411–24. https://doi.org/10.5281/zenodo.5806024.

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Prabhat Engineering College, Kanpur Dehat-209 304, Uuar Pradesh, India <em>E-mail:</em> mksunny63@yahoo.in Saroj Institute of Technology & Management, Lucknow-226 004, Uttar Pradesh, India Department of Chemistry, AI-Margeb University, AI-Khums, Libya V.S.S.D. College, Kanpur-208 002, Uttar Pradesh, India <em>Manuscript received 6 November 2008, revised 15 December 2009, accepted 3 June 2010</em> Halo-substituted arylureas have been .prepared by condensation of halo-substituted primary arylamiue with sodium cyanate and halo-substituted arylthioureu have been prepared by condensation o

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48

Zhang, Ze, Hao-Hao Wu, and Ya-Jun Tan. "Correction: A simple and straightforward synthesis of phenyl isothiocyanates, symmetrical and unsymmetrical thioureas under ball milling." RSC Advances 11, no. 38 (2021): 23418. http://dx.doi.org/10.1039/d1ra90128a.

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Correction for ‘A simple and straightforward synthesis of phenyl isothiocyanates, symmetrical and unsymmetrical thioureas under ball milling’ by Ze Zhang et al., RSC Adv., 2013, 3, 16940–16944, DOI: 10.1039/C3RA43252A.

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49

Jalander, Lars F., and Jan-Erik Lönnqvist. "Synthesis of Alkyl- and Phenyl-2-thiouracils and 1,3-Thiazin-4-ones by Nucleophilic Substitution of Unsymmetrical Thioureas with 3-Chloropropenoates." Collection of Czechoslovak Chemical Communications 64, no. 8 (1999): 1307–15. http://dx.doi.org/10.1135/cccc19991307.

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Unsymmetrically substituted thioureas and ethyl (E)- and (Z)-3-aryl-3-chloro-2-cyano- propenoates (1a) and (1b) gave after nucleophilic vinylic substitution and cyclisation two isomers of 1,3-disubstituted 6-aryl-5-cyano-2-thiouracil derivatives, 3a-3i and 4a-4i. Substituted 1,3-thiazin-4-ones 5a-5d were formed in moderate to good yields when monosubstituted thioureas were allowed to react under similar conditions.

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50

Kholodniak, Olena, and Sergiy Kovalenko. "Substituted acyl thioureas and acyl thiosemicarbazides: synthesis and biological activity (minireview)." ScienceRise: Pharmaceutical Science, no. 2(36) (April 29, 2022): 56–71. http://dx.doi.org/10.15587/2519-4852.2022.255738.

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Acyl isothiocyanates and their functional derivatives (acyl thioureas and acyl thiosemicarbazides) are an important group of organic compounds that are widely used in the synthesis of heterocycles and in chemistry as catalysts, ligands, colorimetric hemosensors, etc. In recent years, there has been an increased interest towards this class of compounds as promising biologically active compounds, especially since the latest advances in medicinal chemistry for them are not sufficiently studied. The aim. To summarize and systematize information for the last 10 years on methods of synthesis a

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