Current Organic Synthesis
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Published By Bentham Science

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2022 ◽  
Vol 19 ◽  
Author(s):  
Pannala Padmaja ◽  
Subba Reddy ◽  
Vinod G. Ugale ◽  
Pedavenkatagari Narayana Reddy

Background: Objective: Objective: biological science.: Background: Arylidenemalononitriles are valuable synthons for the construction of a variety of novel complex heterocyclic motifs, fused heterocycle derivatives and spirocyclic compounds. They are versatile chemical intermediates and have increasing applications in industry, agriculture, medicine, Objective: The aim of this review is to highlight the preparation methods and reactions of arylidenemalononitriles in the synthesis of various heterocyclic compounds. Conclusion: n this review, we have presented the application of arylidenemalononitriles to construct a variety of heterocycles. Various catalysts for the preparation of arylidnemalononitriles have been described.


2022 ◽  
Vol 19 ◽  
Author(s):  
Entesar A. Hassan ◽  
Salem E. Zayed ◽  
Al-Hassan S. Mahdy ◽  
Ahmed M. Abo-Bakr

Background: A series of new pyrimidines and thiazoles containing camphor moiety were synthesized under both conventional and microwave irradiation techniques. Methods: The condensation of camphor either with aminoguanidine or thiosemicarbazide gives the camphor hydrazine carboximidiamide 2 and the camphor thiosemicarbazone 3, respectively. Refluxing of 3 with chloroacetonitrile afforded the camphor thiazol-4-imine 4. Compounds 2 and 4 were used as precursors for the synthesis of target products. Results: The reaction of 2 with different species such as arylidene malononitrile, acetylacetone, and ethyl acetoacetate gave the corresponding camphor pyrimidine derivatives 5a,b-7 while refluxing of compound 4 with different reagents e.g. aldehydes, isatin, ninhydrin, acetic anhydride, benzene sulphonyl chloride, and p-nitro-benzoyl chloride afforded the camphor thiazole derivatives 8a-d-13, respectively. Conclusion: A comparison between the conventional way and the eco-friendly microwave irradiation method occurred in the synthesis of the same compounds, which the latter was more efficient. The elemental analysis, FT-IR, 1H NMR, 13C NMR, and Mass spectra confirm the structures of the obtained new compounds. The potential use of some selected derivatives as antimicrobial agents was investigated and gave promising results


2021 ◽  
Vol 19 ◽  
Author(s):  
Ayushi Singh ◽  
Sibnath Kayal

Background: In today’s world, rising temperature due to global warming is caused by higher concentration of carbon dioxide (CO2) emissions in the atmosphere. Metal-Organic Framework (MOF) materials have the potential to be used in carbon dioxide capture and utilization technology. Objective: The purpose of this work is to prepare metal-organic framework materials by a benign synthesis method using water as the solvent, followed by the characterization and property evaluation for CO2 adsorption study. Methods: MIL-101-Cr metal-organic framework and its derivatives with alkali ion dopants were prepared by benign hydrothermal synthesis route, which were characterized by powder X-ray diffraction method. The adsorption isotherms of CO2 for MIL-101-Cr and its derivatives were studied to comprehend the influence of alkali dopants on CO2 sorption behaviour. The equilibrium uptakes of CO2 were further evaluated by fitting the isotherms with Langmuir, Toth and Dubinin – Astakohv adsorption models to determine the adsorption parameters. Results: The crystalline structural integrity of MIL-101-Cr is not affected by doping with alkali ions. The isosteric heat of CO2 adsorption is diminished with an increase in alkali dopant size, while the induced surface structural heterogeneity increases with increasing alkali dopant size. Conclusion: The equilibrium and thermodynamic parameters calculated from this study are useful for applications in carbon dioxide capture and utilization technology.


2021 ◽  
Vol 19 ◽  
Author(s):  
Fatma A. Mohamed ◽  
Mahmoud B. Sheier ◽  
Maysa M. Reda ◽  
Hassan M. Ibrahim

Aim: The goal of this study is to synthesise, analyse, and employ two new direct dyes based on chromenes derivatives as the chromophoric moiety in dyeing wool, silk, and cotton, with good colour strength, light fastness, and other desirable features. Background: The quest for new direct dyes with antimicrobial qualities for Gram-positive, Gram-negative bacteria, and fungus is underway. These dyes are commonly used on cotton, silk, and wool materials, which have great light fastness, washing, rubbing, and sweating fastness. Methods: Antibacterial activity has been measured for all dyeing fabrics. The parent structure 1 has been synthesized previously as part of the experiment. Then, these dyes are prepared by diazotization followed by coupling reaction, Results and Discussion: The p-Aminobenzenesulfonic acid (C1) and 4-Aminoazobenzene-3,4'-disulfonic acid (C2) are diazotized in hydrochloric acid with sodium nitrite, then coupled with compound 1 in a molar ratio (1: 1) at 250C until the pH is fixed at 5. Finally, the monoazo and diazo direct dyes (D1 and D2) are created. Conclusion: Wool, silk, and cotton materials benefit from the synthetic dyes' increased antibacterial action and dyeing qualities (exhaustion and fixing). They also offer better fastness qualities (light, rubbing, and perspiration).


2021 ◽  
Vol 19 ◽  
Author(s):  
Tangella Nagendra Prasad ◽  
Yeruva Pavankumar Reddy ◽  
Poorna Chandrasekhar Settipalli ◽  
Vadiga Shanthi Kumar ◽  
Eeda Koti Reddy ◽  
...  

Background: 1,2,4-triazoles scaffolds display significant biological activities due to hydrogen bonding, solubility, dipole character, and rigidity Objective: The core motif of 1,2,4-triazoles plays a vital role in clinical drugs such as Rizatriptan (anti-migraine), Ribavirin (antiviral), anastrozole (anticancer), etizolam (anxiolytic), estazolam (anticonvulsant), alprazolam (anti-hypnotic), letrozole (aromatase inhibitor), loreclezole (anticonvulsant), trazadone (antidepressant) etc Method: Epoxide ring opening of tert-butyl 6-oxa-3-azabicyclo [3.1.0] hexane-3-carboxylate followed by methylation under basic conditions and de-protection gave the corresponding trans 1-(4-methoxypyrrolidin-3-yl)-1H-1,2,4-triazole hydrochloride salt as the precursor. This precursor on reaction with substituted benzoyl chlorides and benzyl bromides gave the desired amide and amine products Results: A library of 14 N-substituted pyrrolidine derivatives i.e. trans3-methoxy-4-(1H-1,2,4-triazol-1-yl) pyrrolidin-1-yl) (phenyl)methanone and trans 1-benzyl-4-methoxypyrrolidin-3-yl)-1H-1,2,4-triazole were prepared Conclusion: Eight novel amides (6a-h) and six amines (8a-f) derivatives were synthesized using 1-(4-methoxypyrrolidin-3-yl)-1H-1,2,4-triazole 4 salt with substituted benzoyl chlorides and benzyl bromides.


2021 ◽  
Vol 19 ◽  
Author(s):  
Debasish Kundu ◽  
Anup Roy ◽  
Subir Panja

Abstract: A convenient, efficient, and general procedure for the synthesis of diaryl diselenides has been developed by the reaction of aryl diazonium tetrafluoroborates and Potassium Selenocyanate on the surface of alumina under ball-milling in absence of any solvent, transition metal catalyst and base in room temperature. A wide range of functionalized diaryl diselenides are obtained in high purity and high yield by this procedure. Background: Synthesis of diaryl diselenides was restricted into only few Cu-catalyzed C-Se Cross coupling protocol where use of ligands, high reaction temp, long reaction time were required Objective: To achieve a sustainable protocol for the synthesis of diaryl diselenides Method: Reaction of aryl diazonium fluoroborate with KSeCN was successfully performed under ball milling in absence of any ransition metal catalyst, ligands, base and external heating to get diaryl diselenides. Results: A library of diaryl diselenides were obtained in good yields with different functional groups. Conclusion: First transition metal free protocol for the synthesis of diaryl diselenides has been developed successfully.


2021 ◽  
Vol 19 ◽  
Author(s):  
Nosheen Iqbal ◽  
Ameer Fawad Zahoor ◽  
Nasir Rasool ◽  
Samreen Gul Khan ◽  
Rabia Akhtar ◽  
...  

Background: Tubulysins, linear tetrapeptides show extraordinary cytotoxicity against various cancer cells, with IC50 values in nano or picomolar range. Due to their extremely vigorous anti-proliferative and antiangiogenic characteristics, tubulysins exhibit captivating prospects in the development of anticancer drugs. This review focuses on diverse routes for the total synthesis of natural and synthetic tubulysins as well as their fragments. Objective: The purpose of this review is to present the synthetic strategies for the development of antitumor agents, tubulysins. Conclusion: A range of synthetic pathways adopted for the total synthesis of tubulysins and their fragments have been described in this review. Synthesis of fragments, Tuv, Tup, and Tut can be accomplished by adopting appropriate strategies such as Manganese-mediated synthesis, Ireland-Claisen rearrangement, Mukaiyama aldol reaction, and Mannich process etc. Tubulysin B, D, U, V, and N14-desacetoxytubulysin H have been prepared through Mitsunobu reaction, tert-butanesulfinamide method, Tandem reaction, aza-Barbier reaction, Evans aldol reaction, and C-H activation strategies etc. The remarkable anticancer potential of tubulysins toward a substantiate target make them prominent leads for developing novel drugs against multidrug-resistant cancers.


2021 ◽  
Vol 19 ◽  
Author(s):  
Ergin Keleş ◽  
Burcu Aydıner ◽  
Zeynel Seferoğlu

: Cyanide anion has wide use in industrial areas and high toxic effect on the environment as waste. Moreover, plant seeds contain cyanide which occurs in excessive consumption. Therefore, many studies are carried out to determine cyanide. Especially, optical sensors showing colorimetric and fluorimetric changes have been of considerable interest due to their easy, cheap, and fast responses. This review discusses recent developments in the colorimetric and fluorimetric detection of cyanide by nucleophilic addition to different types of receptors via the chemodosimeter approach. The sensitivity and selectivity of the sensors have been reviewed for changes in absorption and fluorescence, naked-eye detection, real sample application, and detection limits when interacting with cyanide.


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