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1

Petrini, Marino, and Alessandro Palmieri. "Recent Advances in the Synthesis of Unsymmetrical Bisindolylmethane Derivatives." Synthesis 51, no. 04 (2018): 829–41. http://dx.doi.org/10.1055/s-0037-1610349.

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This review article summarizes the fundamental synthetic procedures aimed at the preparation of unsymmetrical bisindolylmethanes that have appeared in the literature since 2010. To this goal, reactive electrophilic indole-containing intermediates are mostly generated from indolylmethanols, indolylmethanamines, and indolylmethanthio derivatives and then made to react with simple or functionalized indoles. The asymmetric synthesis of bisindolylmethanes can be also achieved under chiral-catalyzed conditions.1 Introduction2 Direct Three-Component Coupling3 Reaction of Indolylmethanols4 Reaction of
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2

Jurczak, Janusz, Agnieszka Cholewiak, and Pawel Stepniak. "Linear Neutral Receptors for Anions: Synthesis, Structure and Applications." Synthesis 50, no. 23 (2018): 4555–68. http://dx.doi.org/10.1055/s-0037-1609943.

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A selective digest of linear anion receptors based on different aromatic skeletons is presented. Since the structures of anions vary from one to another, different strategies have been developed over recent years in order to bind anions efficiently and selectively. Rigidity, number of hydrogen bond donors, steric hindrance, and special preorganization of linear receptors are analyzed to shed light on the rational design of anion receptors.1 Introduction2 1,3- and 1,2-Benzene Derivatives3 1,3- and 5,7-Azulene Derivatives4 1,8-Naphthalene Derivatives5 1,8-Anthracene Derivatives6 2,6-Pyridine Der
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3

Kumar, Akhalesh, Rakhi Mishra, Avijit Mazumder, Rupa Mazumder, and Arun Kumar. "An Updated Review on Synthesis and Biological Activities of Thiosemicarbazide Analogs." Asian Journal of Chemistry 33, no. 9 (2021): 1957–75. http://dx.doi.org/10.14233/ajchem.2021.23218.

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This review paper focuses on the different synthetic methodologies that researchers have adopted to synthesize various thiosemicarbazide derivatives with different biological activities of synthesized compounds in the last 20 years. Most of the investigations available in the literature are directed to the biological activities of thiosemicarbazide derivatives with less discussion on its synthetic schemes. This review article presents various reaction scheme, which has been adopted for thiosemicarbazide derivative synthesis along with the reported pharmacological activities of synthesized anal
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4

Smolobochkin, Andrey V., Almir S. Gazizov, Rakhymzhan A. Turmanov, Dinara S. Abdullaeva, Alexander R. Burilov, and Michail A. Pudovik. "N-Phosphorylated Pyrrolidines: An Overview of Synthetic Approaches." Synthesis 52, no. 15 (2020): 2162–70. http://dx.doi.org/10.1055/s-0039-1690889.

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Organophosphorus pyrrolidine derivatives possessing P–N bonds are a promising yet underexplored class of compounds. In this short review we overview the general approaches to these compounds described so far, with a special emphasis on their asymmetric synthesis.1 Introduction2 Synthesis of Pyrrolidine-Based P(III) Derivatives3 Synthesis of Pyrrolidine-Based P(V) Derivatives3.1 Phosphorylation of Pyrrolidines with P(V) Acid Chlorides3.2 Phosphorylation of Pyrrolidines with P(V) Acid Esters3.3 Syntheses via the Atherton–Todd Reaction3.4 Oxidation of Pyrrolidine-Based P(III) Derivatives4 Synthes
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5

Xie, Yang, Zhou Xu, Pei Hu, et al. "Synthesis of the Isodityrosine Moiety of Seongsanamide A–D and Its Derivatives." Marine Drugs 21, no. 7 (2023): 373. http://dx.doi.org/10.3390/md21070373.

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The concise and highly convergent synthesis of the isodityrosine unit of seongsanamide A–D and its derivatives bearing a diaryl ether moiety is described. In this work, the synthetic strategy features palladium-catalyzed C(sp3)–H functionalization and a Cu/ligand-catalyzed coupling reaction. We report a practical protocol for the palladium-catalyzed mono-arylation of β-methyl C(sp3)–H of an alanine derivative bearing a 2-thiomethylaniline auxiliary. The reaction is compatible with a variety of functional groups, providing practical access to numerous β-aryl-α-amino acids; these acids can be co
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6

Sato, Ken-ichi, Shoji Akai, and Juji Yoshimura. "Stereocontrolled Total Synthesis of Tetrodotoxin from myo-Inositol and D-Glucose by Three Routes: Aspects for Constructing Complex Multi-Functionalized Cyclitols with Branched-Chain Structures." Natural Product Communications 8, no. 7 (2013): 1934578X1300800. http://dx.doi.org/10.1177/1934578x1300800726.

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This report describes the stereocontrolled total synthesis of the multi-functionalized cyclitol derivative tetrodotoxin containing eight asymmetric carbons and different types of branched-chains from myo-inositol and D-glucose using three different methods. The tetrodotoxin derivatives possess a relatively small molecular weight but unique structural and chemical properties. Selection of the appropriate synthetic method may be useful not only for compounds related to TTX (including related derivatives) but also for other highly complex multi-functionalized cyclitols containing branched-chains.
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7

Sato, Ken-Ichi, Shoji Akai, and Juji Yoshimura. "Stereocontrolled Total Synthesis of Tetrodotoxin from myo-Inositol and D-Glucose by Three Routes: Aspects for Constructing Complex Multi-Functionalized Cyclitols with Branched-Chain Structures." Natural Product Communications 10, no. 5 (2015): 1934578X1501000. http://dx.doi.org/10.1177/1934578x1501000501.

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This report describes the stereocontrolled total synthesis of the multi-functionalized cyclitol derivative, tetrodotoxin, containing eight asymmetric carbons and different types of branched-chains, from myo-inositol and D-glucose using three different methods. The tetrodotoxin derivatives possess a relatively small molecular weight but unique structural and chemical properties. Selection of the appropriate synthetic method may be useful not only for compounds related to TTX (including related derivatives), but also for other highly complex multi-functionalized cyclitols containing branched-cha
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8

Kanazawa, Junichiro, and Masanobu Uchiyama. "Recent Advances in the Synthetic Chemistry of Bicyclo[1.1.1]pentane." Synlett 30, no. 01 (2018): 1–11. http://dx.doi.org/10.1055/s-0037-1610314.

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Utilization of three-dimensional cyclic scaffolds is important in modern drug discovery, both to provide greater opportunities for optimizing drug candidates and to expand the available chemical space of drugs. Among these scaffolds, bicyclo[1.1.1]pentane (BCP) is a high-value bioisostere for 1,4-disubstituted phenyl rings, internal alkynes, and the tert-butyl group, generally offering high passive permeability, high water solubility, and improved metabolic stability. However, the lack of methods for functionalizing BCP remains a significant challenge, and in particular, a versatile strategy f
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9

Tschakert, Jochen, and Wolfgang Voelter. "Festphasensynthese von Muramyldipeptidderivaten und Untersuchung ihrer biologischen Aktivität / Solid Phase Synthesis of Muramyl Dipeptide Derivatives and Investigations on their Biological Activities." Zeitschrift für Naturforschung B 49, no. 5 (1994): 702–16. http://dx.doi.org/10.1515/znb-1994-0524.

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New muramyl dipeptide derivatives with exchanged carbohydrate residues are described. Each derivative is synthesized via a solid phase synthesis using an aminomethyl anchor resin. All synthetic products can be isolated in good yields. Their biological activities are tested by the luminol-dependent chemiluminescence associated with the phagocytosis of opsonized zymosan by granulocytes.
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10

LÓPEZ LÓPEZ, Lluvia Itzel, Sendar Daniel NERY FLORES, Sonia Yesenia SILVA BELMARES, and Aidé SÁENZ GALINDO. "Naphthoquinones: biological properties and synthesis of lawsone and derivates - a structured review." Vitae 21, no. 3 (2014): 248–58. http://dx.doi.org/10.17533/udea.vitae.17322.

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Background: Naphthoquinones are natural pigments that are widely distributed in nature and have important biological activities. Lawsone (2-hydroxy-1,4-naphthoquinone) and its synthetic derivatives, and especially those containing nitrogen, have promising potential for the treatment of different diseases due to their antibacterial, antifungal, antiviral, antitumor and antiparasitic effects, and for pest control via their molluscicidal and insecticidal activities. Their pharmacological activities and mechanisms of action are related to their oxide/reduction and acid/base properties, and can be
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11

MISHRA, KHUSHBOO, S. K. Jain, and P. K. Singour. "Synthesis and Biological Evaluation of pyrazole derivatives containing ethanone skeleton as Anti-inflammatory agents." Journal of Drug Delivery and Therapeutics 9, no. 3 (2019): 40–47. http://dx.doi.org/10.22270/jddt.v9i3.2736.

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Current research had focused on the synthesis of the novel pyrazole ethanone linked compounds with improved biological activity. In this synthetic process 1st step was to synthesize the intermediate chalcone and 2nd step was the synthesis of final compound pyrazole derivative containing ethanone moiety. This procedure is the type of cyclization reaction using proton transfer mechanism. By using this method 8 derivatives synthesized. After synthesis these were subjected to identification tests by using various methods like melting point study, thin layer chromatography, solubility study and cha
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12

Iqbal, Dure Najaf, Arif Nazir, Munawar Iqbal, and Muhammad Yameen. "Green synthesis and characterization of carboxymethyl guar gum: Application in textile printing technology." Green Processing and Synthesis 9, no. 1 (2020): 212–18. http://dx.doi.org/10.1515/gps-2020-0022.

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AbstractThis study focusses on the synthesis of carboxymethyl guar gum (CMG) via monochloroacetic acid under alkaline conditions. The reaction conditions were also optimized during the course of experiment. Guar derivative with variable degree of substitution (DS) were prepared and were confirmed by Fourier transform infrared (FTIR) spectroscopy. The DS was determined quantitatively by titration method for each derivative. The synthesized guar gum derivatives, being the natural thickners, have been used in textile printing technology. Substituted guar gum has been proved environmental friendly
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13

Riaz, Sharon, Khalid Mohammed Khan, Ghayoor Abbas Chotana, Amir Faisal, and Rahman Shah Zaib Saleem. "The Antimitotic Podophyllotoxin and its Derivatives Recent Synthetic Advances." Current Nutraceuticals 3, no. 1 (2022): 4–37. http://dx.doi.org/10.2174/2665978602666211102103152.

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: The substantial antimitotic potential of podophyllotoxin and its derivatives has attracted both synthetic and medicinal chemists to expand the chemical space for the subsequent biological evaluation of these compounds. The interest ranges from total synthesis, hemi-synthesis, one-pot synthetic approaches and structure-activity relationship studies. In the first segment of the review, we present recent development in the synthesis of podophyllotoxin and also describe its mode of action. the second section covers the synthesis and the structure-activity relationships of podophyllotoxin derivat
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14

Rohi, Marziyeh, Bahareh Sadeghi та Mohamadhosaine Moslemin. "Synthesis of spirooxindoles with three component reaction between β-ketoesters, malononitrile and isatin derivatives in the presence of Alum.SiO2 nanoparticles as a new nano catalyst". Ciência e Natura 37 (21 грудня 2015): 80. http://dx.doi.org/10.5902/2179460x20834.

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In this reseaech, some of the spirooxindole derivaties were prepared via β-ketoesters, malonoitrile and isatin derivatives in the presenceAlum.SiO2 NPs as an effective, recyclable and inexpensive catalyst. The products were identified by IR, 1HNMR, 13C NMR spectr a, andmelting point. The size of nanoparticles characterized by SEM and TEM techniques. A novel multicomponent synthesis of a series ofspirooxindol derivatives is described. The procedures was carried out applying Alum/SiO2 supported on NPS as the novel cataly st givingrise to high to excellent yielded synthetic route of spirooxindol
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15

Guan, Jinming, Matthew Hachey, Lekha Puri, Vanessa Howieson, Kevin J. Saliba, and Karine Auclair. "A cross-metathesis approach to novel pantothenamide derivatives." Beilstein Journal of Organic Chemistry 12 (May 13, 2016): 963–68. http://dx.doi.org/10.3762/bjoc.12.95.

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Pantothenamides are known for their in vitro antimicrobial activity. Our group has previously reported a new stereoselective route to access derivatives modified at the geminal dimethyl moiety. This route however fails in the addition of large substituents. Here we report a new synthetic route that exploits the known allyl derivative, allowing for the installation of larger groups via cross-metathesis. The method was applied in the synthesis of a new pantothenamide with improved stability in human blood.
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16

Shoji, Taku, Mutsumi Takeuchi, Mayumi Uda, et al. "Synthesis of Azuleno[2,1-b]quinolones and Quinolines via Brønsted Acid-Catalyzed Cyclization of 2-Arylaminoazulenes." Molecules 28, no. 15 (2023): 5785. http://dx.doi.org/10.3390/molecules28155785.

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Quinolone and quinoline derivatives are frequently found as substructures in pharmaceutically active compounds. In this paper, we describe a procedure for the synthesis of azuleno[2,1-b]quinolones and quinolines from 2-arylaminoazulene derivatives, which are readily prepared via the aromatic nucleophilic substitution reaction of a 2-chloroazulene derivative with several arylamines. The synthesis of azuleno[2,1-b]quinolones was established by the Brønsted acid-catalyzed intramolecular cyclization of 2-arylaminoazulene derivatives bearing two ester groups at the five-membered ring. The halogenat
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17

Gaonkar, Santosh L., Vignesh U. Nagaraj, and Swarnagowri Nayak. "A Review on Current Synthetic Strategies of Oxazines." Mini-Reviews in Organic Chemistry 16, no. 1 (2018): 43–58. http://dx.doi.org/10.2174/1570193x15666180531092843.

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In the past three decades, the heterocyclic oxazine cores have been intensely concerned. Oxazine derivatives are promising vital heterocyclic motifs. They are eminent for their synthetic potential and extensive biological properties. Oxazines are versatile intermediates for the synthesis of a variety of heterocycles and bifunctional compounds. Researchers have reported several synthetic approaches for the preparation of oxazines. This review emphasises the recent approaches for the synthesis of oxazine derivatives.
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18

Huang, Y., Z. Jiang, X. Liao, J. Hou, and X. Weng. "Antioxidant activities of two novel synthetic methylbenzenediol derivatives ." Czech Journal of Food Sciences 32, No. 4 (2014): 348–53. http://dx.doi.org/10.17221/283/2013-cjfs.

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2-(tert-Butyl)-5-methylbenzene-1,4-diol and 3-(tert-butyl)-5-methylbenzene-1,2-diol were synthesised by Friedel-Craft reaction of 2-methylbenzene-1,4-diol and 4-methylbenzene-1,2-diol, respectively, with tertiary butanol providing reasonable yields. The antioxidant activities of these two products, mother compounds and 2-(tert-butyl)benzene-1,4-diol were investigated and compared by means of 2,2-diphenyl-1-picrylhydrazyl radical and Rancim at test; 3-(tert-butyl)-5-methylbenzene-1,2-diol is the most potent antioxidant tested by using Rancimat test experiment. The 2,2-diphenyl-1-picrylhydrazyl
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19

Żurawiński, Remigiusz, Marian Mikołajczyk, Marcin Cieślak, Karolina Królewska, and Julia Kaźmierczak-Barańska. "Synthesis and in vitro cytotoxicity of cross-conjugated prostaglandin A and J series and their hydroxy derivatives." Organic & Biomolecular Chemistry 13, no. 25 (2015): 7000–7012. http://dx.doi.org/10.1039/c5ob00550g.

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20

P., RAJANI, ASHOK D., and N. SARMA P. "Synthetic Experiments on Pongamol." Journal of Indian Chemical Society Vol. 68, Jan 1991 (1991): 52–55. https://doi.org/10.5281/zenodo.5968139.

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Department of Chemistry, Osmania University, Hyderabad-500 007 <em>Manuscript received&nbsp;5 October 1990, accepted 14 January 1991</em> A number of new pyrazole and isoxazole derivatives have been synthesised starting from pongamol a naturally occurring benzofuran derivative containing 1,3-diketone system. All the compounds have been characterised by their analytical and spectral data and were screened for their antifeedant activity,
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21

Moreira, Natália Menezes, Lorena Suelen Ribeiro Martelli, and Arlene Gonçalves Corrêa. "Asymmetric organocatalyzed synthesis of coumarin derivatives." Beilstein Journal of Organic Chemistry 17 (August 3, 2021): 1952–80. http://dx.doi.org/10.3762/bjoc.17.128.

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Coumarin derivatives are essential scaffolds in medicinal and synthetic chemistry. Compounds of this class have shown important activities, such as anticancer and antiparasitic, besides the commercially available drugs. These properties led to the development of efficient and greener synthetic methods to achieve the 2H-chromen-2-one core. In this context, the advances in asymmetric organocatalyzed synthesis of coumarin derivatives are discussed in this review, according to the mode of activation of the catalyst.
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22

Valík, Martin, Bohumil Dolensky, Hana Petříčková, and Vladimír Král. "Regio- and Stereoselectivity in Preparation of Benzene Bridged Bis- and Tris-Tröger's Bases." Collection of Czechoslovak Chemical Communications 67, no. 5 (2002): 609–21. http://dx.doi.org/10.1135/cccc20020609.

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Synthetic strategy for novel multiple Tröger's base derivatives is presented. Compounds were prepared in three steps: o-nitrobenzoylation of benzene-1,2- and -1,3-diamines 3 followed by reduction of nitro and amide groups to amino functions and treatment of the obtained tetraamine compounds 6 with formaldehyde lead to simultaneous formation of bis-Tröger's base (bisTB) derivatives 7a, 7b. Only products of 1,2,3,4-substituted regioisomers with anti conformation were separated from reaction mixtures. The same synthetic procedure was used for preparation of tris-Tröger's base (trisTB) derivative
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23

Fernandes, Carla, Maria Carraro, João Ribeiro, Joana Araújo, Maria Tiritan, and Madalena Pinto. "Synthetic Chiral Derivatives of Xanthones: Biological Activities and Enantioselectivity Studies." Molecules 24, no. 4 (2019): 791. http://dx.doi.org/10.3390/molecules24040791.

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Many naturally occurring xanthones are chiral and present a wide range of biological and pharmacological activities. Some of them have been exhaustively studied and subsequently, obtained by synthesis. In order to obtain libraries of compounds for structure activity relationship (SAR) studies as well as to improve the biological activity, new bioactive analogues and derivatives inspired in natural prototypes were synthetized. Bioactive natural xanthones compromise a large structural multiplicity of compounds, including a diversity of chiral derivatives. Thus, recently an exponential interest i
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24

Havránková, Eva, Jozef Csöllei, and Pavel Pazdera. "New Approach for the One-Pot Synthesis of 1,3,5-Triazine Derivatives: Application of Cu(I) Supported on a Weakly Acidic Cation-Exchanger Resin in a Comparative Study." Molecules 24, no. 19 (2019): 3586. http://dx.doi.org/10.3390/molecules24193586.

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An efficient and simple methodology for Ullmann Cu(I)-catalyzed synthesis of di- and trisubstituted 1,3,5-triazine derivatives from dichlorotriazinyl benzenesulfonamide and corresponding nucleophiles is reported. Cations Cu(I) supported on macroporous and weakly acidic, low-cost industrial resin of polyacrylate type were used as a catalyst. The reaction times and yields were compared with traditional synthetic methods for synthesis of substituted 1,3,5-triazine derivatives via nucleophilic substitution of chlorine atoms in dichlorotriazinyl benzenesulfonamide. It was found that Ullmann-type re
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25

Gomes, Claudia R. B., Marcus V. N. de Souza, and Victor Facchinetti. "A Review on Onychine and its Analogs: Synthesis and Biological Activity." Current Organic Synthesis 17, no. 1 (2020): 3–22. http://dx.doi.org/10.2174/1570179417666191218112842.

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Background: Onychine is a 4-azafluorenone alkaloid isolated from the Annonaceae family, in low concentrations. Onychine and its analogs exhibit a wide range of pharmacological activities such as antifungal, antibacterial, anticancer, and antimalarial. Because of the high bioactivity of some 4-azafluorenone derivatives, several synthetic methods have been developed for their procurement. Objective: Considering the importance of these alkaloids, we aim to present the main synthetic approaches to onychines and its derivatives and the biological activity of some 4-azafluorenones. Methods: The most
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26

Raju, Gali Pushpa, Sailaja Gugulothu, and Khasim Sharif Syed. "Biological significance and synthetic approaches for 1,3,4-Thiadiazoles: A Review." Caribbean Journal of Science and Technology 07, no. 01 (2019): 15–21. http://dx.doi.org/10.55434/cbi.2019.7101.

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In this article the authors presented a short review of literature survey on the synthetic approaches for the synthesis of thiadiazoles and their derivatives. Further, various biological activities of these derivatives were also summarized.
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27

Khadieva, Alena, Mansur Rayanov, Ksenia Shibaeva, Alexandr Piskunov, Pavel Padnya, and Ivan Stoikov. "Towards Asymmetrical Methylene Blue Analogues: Synthesis and Reactivity of 3-N′-Arylaminophenothiazines." Molecules 27, no. 9 (2022): 3024. http://dx.doi.org/10.3390/molecules27093024.

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The search for new ways to obtain analogues of the well-known Methylene Blue dye is an important synthetic task. Herein, we proposed and developed an approach to the synthesis of 3-N′-arylaminophenothiazines and asymmetrical 3,7-di(N′-arylamino)phenothiazines. This approach included the optimization of synthetic strategy by quantification analysis of the positive charge distribution in the cation of 3-N′-arylaminophenothiazine derivative. The obtained experimental data are confirmed by DFT studies. Two synthetic routes for asymmetrical phenothiazine diarylamino derivatives were suggested and v
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28

Somarouthu, Veeraswamy. "Chemistry and pharmacological activities of Thiazoles –A Review Update." Caribbean Journal of Science and Technology 07, no. 01 (2019): 28–37. http://dx.doi.org/10.55434/cbi.2019.7102.

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This mini-review presents a summary of literature survey on the synthetic approaches for the synthesis of thiazoles and their derivatives. Further, various biological activities of these derivatives were also summarized.
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29

Hasan Mohammed Marhoon and Ezzat Hussein Zimam. "Synthesis and antibacterial screening of some new 1'2'3 -triazole derivatives from dapsone." Journal of Kufa for Chemical Sciences 3, no. 2 (2024): 129–51. http://dx.doi.org/10.36329/jkcm/2024/v3.i2.12586.

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In our relentless pursuit of developing innovative antibacterial derivatives, we have successfully generated and evaluated a novel series of 1,2,3-triazole derivatives derived from azo dapsone. The synthesis process commenced with the fusion of the dapsone core with the triazole framework, establishing a solid foundation for our synthetic endeavors. Subsequently, the azo dapsone nucleus underwent functionalization using sodium azide, resulting in the creation of an azide derivative (B). To synthesize the desired end 1,2,3-triazoles, a click reaction was employed, combining the azide compound w
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30

Prakash, Gaurav, Ajay Kumar Das, and V. D. Tripathi. "A Catalyst Free and Sustainable Synthesis of Quinazolinones in Glycerol as Green Solvent." Asian Journal of Chemistry 35, no. 5 (2023): 1089–94. http://dx.doi.org/10.14233/ajchem.2023.27612.

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In this article, glycerol was employed in a quest to develop an environmentally benign and sustainable synthetic protocol for synthesis of quinazolinone and spiro-quinazolinone derivatives. These studies were performed to investigate the effect of electron-rich and electronegative groups on the synthetic route of an established protocol. Different substituted isatin and benzaldehyde derivatives have been incorporated to synthesize analogues of two series of quinazolinones in order to investigate the efficacy of the developed methodology and substrate tolerance. A total of 12 derivatives were s
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31

Tejeswararao, D. "Diversity and Oriented Synthesis of Clopidogrel Drug Derivatives." Asian Journal of Chemistry 32, no. 12 (2020): 3007–11. http://dx.doi.org/10.14233/ajchem.2020.22881.

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An efficient synthetic route has been developed for the synthesis of new clopidogrel drug derivatives. Key step of this method is to replacement of mesyl protected alcohol group with various aliphatic amines in presence of base. Various clopidogrel drug derivatives have been prepared in good yields. All the new compounds were confirmed by spectral studies and mass analysis. The main advantage of the new synthetic route has low cost and is fit for industrial applications.
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32

Molnar, Maja, Melita Lončarić, and Marija Kovač. "Green Chemistry Approaches to the Synthesis of Coumarin Derivatives." Current Organic Chemistry 24, no. 1 (2020): 4–43. http://dx.doi.org/10.2174/1385272824666200120144305.

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This review is a compilation of the green synthetic methods used in the synthesis of coumarin derivatives. Coumarins are a class of compounds with a pronounced wide range of biological activities, which have found their application in medicine, pharmacology, cosmetics and food industry. Their biological activity and potential application are highly dependent on their structure. Therefore, many researchers have been performing the synthesis of coumarin derivatives on a daily basis. High demands for their synthesis often result in an increased generation of different waste chemicals. In order to
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33

Singh, Nidhi, Krishna Rajotiya, Nikita Lamba, H. L. Singh, K. L. Ameta, and Shivendra Singh. "Versatile Approach for the Synthesis of Furo-coumarin Derivatives." Current Organic Chemistry 26, no. 3 (2022): 324–41. http://dx.doi.org/10.2174/1385272826666220126155703.

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Abstract: Owing to useful physio-chemical properties of furo-coumarin derivatives, their synthetic and mechanistic investigation has been reported here. We have demonstrated a range of synthetic approaches to access furan-fused coumarin derivatives. Many metalmediated, base, and acid-catalyzed approaches have been revealed for the formation of this coumarin-based fused heterocycles of biological importance. In addition to this, microwaveassisted synthetic routes have also been revealed. The last and most useful approach for the synthesis of these heterocycles includes the use of purely solvent
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34

Acosta-Quiroga, Karen, Cristian Rojas-Peña, Luz Stella Nerio, Margarita Gutiérrez, and Efraín Polo-Cuadrado. "Spirocyclic derivatives as antioxidants: a review." RSC Advances 11, no. 36 (2021): 21926–54. http://dx.doi.org/10.1039/d1ra01170g.

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35

Chamni, Supakarn, Natchanun Sirimangkalakitti, Pithi Chanvorachote, Khanit Suwanborirux, and Naoki Saito. "Chemistry of Renieramycins. Part 19: Semi-Syntheses of 22-O-Amino Ester and Hydroquinone 5-O-Amino Ester Derivatives of Renieramycin M and Their Cytotoxicity against Non-Small-Cell Lung Cancer Cell Lines." Marine Drugs 18, no. 8 (2020): 418. http://dx.doi.org/10.3390/md18080418.

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Two new series of synthetic renieramycins including 22-O-amino ester and hydroquinone 5-O-amino ester derivatives of renieramycin M were semi-synthesized and evaluated for their cytotoxicity against the metastatic non-small-cell lung cancer H292 and H460 cell lines. Interestingly, the series of 22-O-amino ester derivatives displayed a potent cytotoxic activity greater than the hydroquinone derivatives. The most cytotoxic derivative of the series was the 22-O-(N-Boc-l-glycine) ester of renieramycin M (5a: IC50 3.56 nM), which showed 7-fold higher potency than renieramycin M (IC50 24.56 nM) and
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36

OLIVEIRA, Saulo Pomponet, Alessandra de Barros e. Silva BONGIOLO, Luan Thanh PHAM, Luís Gustavo DE CASTRO, and Vinicius Theobaldo JORGE. "On the practical implementation of the enhanced horizontal derivative filter for potential field data." Contributions to Geophysics and Geodesy 53, no. 4 (2023): 319–31. http://dx.doi.org/10.31577/congeo.2023.53.4.1.

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The enhanced horizontal derivative (EHD) is an enhancement filter whose maxima provide estimated locations of the sources' boundaries. This filter is defined as the total horizontal derivative (THDR) of a weighted sum of vertical derivatives of increasing order. We consider some aspects of the practical implementation of the EHD filter, especially its robustness. A slightly different version of EHD, which we refer to as mEHD, is obtained when we switch the order of THDR and the weighted sum; that is, when we consider the weighted sum of total horizontal derivatives of the successive vertical d
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37

Zuhdi, Muhammad, Bakti Sukrisna, and Syamsuddin Syamsuddin. "IDENTIFICATION OF BURIED ARCHEOLOGICAL OBJECTS WITH RADIAL DERIVATIVES OF MICRO GRAVITY DATA." Indonesian Physical Review 2, no. 2 (2019): 84. http://dx.doi.org/10.29303/ipr.v2i2.25.

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The development of recent gravimetric technology allows us to measure gravity anomalies with accuracy of micro Gal. Micro gravity is able to detect very small gravity anomalies such as anomaly due to buried archeological objects below the earth surface. Radial Derivatives of gravity data is used to sharpen anomaly due to lateral changes of density contrast. Horizontal derivatives carried out by previous researchers have some weaknesses, i.e. the loss of derivative values in certain directions and inconsistence values at the source boundary of the same anomaly edge. To solve the horizontal deri
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38

Queda, Fausto, Gonçalo Covas, Sérgio Filipe, and M. Marques. "Assembly of Peptidoglycan Fragments—A Synthetic Challenge." Pharmaceuticals 13, no. 11 (2020): 392. http://dx.doi.org/10.3390/ph13110392.

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Peptidoglycan (PGN) is a major constituent of most bacterial cell walls that is recognized as a primary target of the innate immune system. The availability of pure PGN molecules has become key to different biological studies. This review aims to (1) provide an overview of PGN biosynthesis, focusing on the main biosynthetic intermediates; (2) focus on the challenges for chemical synthesis posed by the unique and complex structure of PGN; and (3) cover the synthetic routes of PGN fragments developed to date. The key difficulties in the synthesis of PGN molecules mainly involve stereoselective g
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39

Moetlediwa, Marakiya T., Babalwa U. Jack, Sithandiwe E. Mazibuko-Mbeje, et al. "Evaluating the Therapeutic Potential of Curcumin and Synthetic Derivatives: A Computational Approach to Anti-Obesity Treatments." International Journal of Molecular Sciences 25, no. 5 (2024): 2603. http://dx.doi.org/10.3390/ijms25052603.

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Natural compounds such as curcumin, a polyphenolic compound derived from the rhizome of turmeric, have gathered remarkable scientific interest due to their diverse metabolic benefits including anti-obesity potential. However, curcumin faces challenges stemming from its unfavorable pharmacokinetic profile. To address this issue, synthetic curcumin derivatives aimed at enhancing the biological efficacy of curcumin have previously been developed. In silico modelling techniques have gained significant recognition in screening synthetic compounds as drug candidates. Therefore, the primary objective
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40

Avhad, Datta, Alpana Asnani, Shrikant Mohurle, Pratyush Kumar, Abhibnav Bais, and Ruchita Tale. "Review on synthetic study of benzotriazole." GSC Biological and Pharmaceutical Sciences 11, no. 2 (2020): 215–25. https://doi.org/10.5281/zenodo.4274541.

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Benzotriazole is nitrogen containing heterocycle derivative containing three nitrogen atoms at 1st, 2nd, 3 rd positions. Lone pairs of each nitrogen atom are present in unshared form. The unshared lone pair of electrons enables five-membered ring to exhibit that can exist in tautomeric forms. Benzotriazole belongs to a fused heterocycles, which has a benzene ring fused with with a traizole ring. Benzotriazole and its derivatives have great significance in medicinal chemistry. The derivatives are used by several chemists for therapeutic conditions. The current paper concise several synthetic me
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41

Shu, Penghua, Haichang Xu, Lingxiang Zhang, et al. "Synthesis of (Z)-Cinnamate Derivatives via Visible-Light-Driven E-to-Z Isomerization." SynOpen 03, no. 04 (2019): 103–7. http://dx.doi.org/10.1055/s-0039-1690331.

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(Z)-Cinnamate derivatives are prevalent in natural bioactive products and in organic synthesis. Herein, we report a practical approach toward the efficient synthesis of (Z)-cinnamate derivatives via visible-light-driven isomerization. When E-isomers of cinnamate derivatives were irradiated with blue light in the presence of 1 mol% Ir2(ppy)4Cl2 (ppy = 2-phenylpyridine), Z-isomers were readily obtained in good yields. This strategy allows the large-scale synthesis of (Z)-cinnamate derivatives with simple purification. This convenient, mild, and green synthetic methodology was subsequently applie
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Kotha, Sambasivarao, Kakali Lahiri, and Gaddamedi Sreevani. "Design and Synthesis of Aromatics through [2+2+2] Cyclotrimerization." Synlett 29, no. 18 (2018): 2342–61. http://dx.doi.org/10.1055/s-0037-1609584.

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The [2+2+2] cycloaddition reaction is a useful tool to realize unusual chemical transformations which are not achievable by traditional methods. Here, we report our work during the past two decades that involve utilization of transition-metal complexes in a [2+2+2] cyclotrimerization reaction. Several key “building blocks” were assembled by a [2+2+2] cycloaddition approach and they have been further expanded by other synthetic transformations to design unusual amino acids and peptides, diphenylalkanes, bis- and trisaryl benzene derivatives, annulated benzocycloalkanes, spirocycles, and spiroox
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Patel, Krina, Heli Patel, Drashti Shah, et al. "Unlocking the Potential: A Comprehensive Review for the Synthesis of Benzofuran Derivatives." Current Green Chemistry 11, no. 1 (2024): 12–36. http://dx.doi.org/10.2174/0122133461272081231102061911.

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Abstract: Benzofuran, a versatile heterocyclic compound, has gained considerable attention in recent years due to its diverse biological activities, distinctive structural characteristics, broad synthetic approaches, and extensive applications. The growing potential inherent in benzofuran encourages many researchers to address the challenges of the synthesis of its framework. This comprehensive review aims to provide a detailed overview of the recent advancements in the synthesis of diverse benzofuran derivatives, highlighting innovative strategies, synthetic methodologies, and significant bre
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Roller, Clara A., Berenike Doler, and Roland C. Fischer. "Preparation and Structural Variety of Neutral Heptaphospha-Nortricyclane Derivatives of Zinc and the Coinage Metals." Crystals 14, no. 7 (2024): 586. http://dx.doi.org/10.3390/cryst14070586.

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In this study, we report the preparation of neutral Au(I), Ag(I), and Cu(I) derivatives [(hyp)2P7M]n (M = Au, n = 2; M = Ag, Cu, n = 4) of a heptaphospha-nortricyclane cage. Synthesis was conducted via a halodesilylation route under the cleavage of the sterically less shielded trimethyl silyl group, starting from the heteroleptic cage (hyp)2(tms)P7. All coinage metal derivatives exhibit short metal–metal distances of 2.9542(2) Å (Au), 2.8833(6) Å (Ag), and 2.654(1) Å (Cu), respectively. The same synthetic methodology was also applied for the preparation of a zinc derivative, [{(hyp)2P7}2Zn]*Et
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Chrzanowska, Maria, Agnieszka Grajewska, and Maria D. Rozwadowska. "Diastereoselective Synthesis of (–)-6,7-Dimethoxy-1,2,3,4-tetrahydroisoquinoline-1-carboxylic Acid via Morpholinone Derivatives." Molecules 28, no. 7 (2023): 3200. http://dx.doi.org/10.3390/molecules28073200.

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A simple and convenient synthesis of (–)-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline-1-carboxylic acid is described, applying a combination of two synthetic methods: the Petasis reaction and Pomeranz–Fritsch–Bobbitt cyclization. The diastereomeric morpholinone derivative N-(2,2-diethoxyethyl)-3-(3,4-dimethoxyphenyl)-5-phenyl-1,4-oxazin-2-one formed in the Petasis reaction was further transformed into 1,2,3,4-tetrahydroisoquinoline-1-carboxylic acid via Pomeranz–Fritsch–Bobbitt cyclization, a classical method of synthesis leading to the tetrahydroisoquinoline core. We review important examples
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NITYA, ANAND, JAIN SANJAY, and SINHA NEELIMA. "Molecular Diversity Generation through Reactive Lactams." Journal of Indian Chemical Society Vol. 74, Nov-Dec 1997 (1997): 948–54. https://doi.org/10.5281/zenodo.5900789.

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Central Drug Research Institute, Lucknow-226 001 Medicinal Chemistry- Division, NDDR, Ranbaxy Research Laboratroy, A-1, Phase-I, Okhla Industrial Area, New Delhi-110 020 <em>Manuscript received 6 October 1997</em> Generation of combinatorial libraries has come to occupy a central stage in the search for novel lead structures/ pharmacophores needed for new drug discovery research through molecular diversity. In the creation of molecular diversity by synthesis, the synthetic strategies should be short-path, convergent, high yielding and amenable to be carried out under mild conditions. Activated
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Zhu, Yue, Xu Yao, Jin Long, et al. "Fluorine-Containing Chrysin Derivatives." Natural Product Communications 14, no. 9 (2019): 1934578X1987892. http://dx.doi.org/10.1177/1934578x19878921.

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Chrysin, a flavonoid, has played a great role in the fields of anticancer, antibacterial, and antiviral drug discovery. A large number of chrysin derivatives have been synthesized recently. The fluorine atom represents an important substituent group for a great number of natural products and pharmaceuticals. Taking into account the importance of both chrysin and the fluorine atom in medicinal chemistry, the synthesis of fluorine-containing chrysin derivatives has gained great interest. Chemically, the synthetic methods for these new chrysin derivatives have also been developed rapidly. In rece
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Soares, Ana Carolina Ferreira, Priscilla Mendonça Matos, Herbert Júnior Dias, et al. "Variability of the antibacterial potential among analogue diterpenes against Gram-positive bacteria: considerations on the structure–activity relationship." Canadian Journal of Chemistry 97, no. 7 (2019): 568–75. http://dx.doi.org/10.1139/cjc-2018-0369.

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The search for new antibacterial agents and a better comprehension of substances with antimicrobial behavior is mandatory nowadays due to the serious public health problem of infection diseases. In the present work, 30 diterpenes were studied, with 2 natural derivatives, named ent-16-kauren-19-oic acid and ent-pimara-8(14),15-dien-19-oic acid, and 28 semi-synthetic derivatives. The natural diterpenes were isolated from Mikania glomerata and Viguiera arenaria, respectively. All diterpenes were submitted to antimicrobial assays against six different Gram-positive microorganisms to better underst
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Sanaryh Mohammed Al-awad, Leaqaa Abdalredha raheem, and Ausama Ayob Jaccob. "Synthesis and Pharmacological Evaluation of Novel Coumarin Derivatives." International Journal of Research in Pharmaceutical Sciences 11, no. 1 (2020): 865–74. http://dx.doi.org/10.26452/ijrps.v11i1.1908.

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The current work focuses on new architecture, synthesis of coumarin-oxadiazole hybrid derivative products as both these (coumarin ring and oxadiazole) have a wide variety of biological behavior, Compounds containing the nucleus of coumarin (2H-1-benzopyran-2-one) are an interesting class of hetero cycles which hold an important role in the field of natural ingredients and synthetic organic chemistry. It has been exciting medicinal chemists to study native coumarins or synthetic analogs for their application for decades. And they can be further modified to synthesize more effective and potent d
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50

Sadek, Kamal Usef, Ramadan Ahmed Mekheimer, and Mohamed Abd-Elmonem. "Recent Developments in the Synthesis of Cinnoline Derivatives." Mini-Reviews in Organic Chemistry 16, no. 6 (2019): 578–88. http://dx.doi.org/10.2174/1570193x15666180712124148.

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Crinnolines can serve as unique and versatile class of heterocycles especially in fields related to synthetic and pharmaceutical chemistry owing to their potent biological activities. They possess diversity of pharmaceutical activities as anticancer, antibacterial, anti-inflammatory, anti-allergic as well as anti-hypertensive activities. Since the first synthesis of cinnoline by Richter (1883) numerous protocols for their synthesis have been developed utilizing arenediazonium salts, aryl hydrazines and arylhydhydrazones precursors. Recently metal catalyzed C-C and C-N bond formation reactions
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