scholarly journals Microwave-Assisted Expeditious Synthesis of 2-Alkyl-2-(N-arylsulfonylindol-3-yl)-3-N-acyl-5-aryl-1,3,4-oxadiazolines Catalyzed by HgCl2 under Solvent-Free Conditions as Potential Anti-HIV-1 Agents

Molecules ◽  
2018 ◽  
Vol 23 (11) ◽  
pp. 2936 ◽  
Author(s):  
Zhiping Che ◽  
Yuee Tian ◽  
Shengming Liu ◽  
Jia Jiang ◽  
Mei Hu ◽  
...  
Keyword(s):  
Large Scale ◽  
Reaction Times ◽  
Solvent Free ◽  
Catalyst Loading ◽  
Microwave Assisted ◽  
Solvent Free Conditions ◽  
Large Scale Synthesis ◽  
Low Catalyst Loading ◽  
Anti Hiv ◽  
Hiv 1

A series of 2-alkyl-2-(N-arylsulfonylindol-3-yl)-3-N-acyl-5-aryl-1,3,4-oxadiazolines were expeditious prepared under microwave-assisted, catalyzed by HgCl2 and solvent-free conditions. This method has the advantage of low catalyst loading and recovering catalyst, ease reaction and repaid reaction times, easy separation products and excellent yields, and more conducive to the large-scale synthesis products. Furthermore, compounds 3s, 3y, 3a′, 3b′, 3f′, 3i′, 3q′, and 3r′ exhibited more potent anti-HIV-1 activity with EC50 values of 3.35, 6.12, 3.63, 9.54, 1.79, 0.51, 3.00, and 4.01 μg/mL, and TI values of 32.66, >32.68, 31.22, 13.94, 24.27, 39.59, 26.01, and 24.51, respectively. Especially compound 3i′ displayed the highest anti-HIV-1 activity with TI values of 39.59.

scholarly journals Silica Supported Acids (SiO2-HClO4, SiO2-KHSO4) as Eco-friendly Reusable Catalysts for Bromination of Aromatic and Heteroaromatic Compoundsusing Kbr Under Solvothermal and Solvent-free Conditions

2021 ◽  
Author(s):  
Vijayshekar pulusu ◽  
Chinna Rajanna Rajanna Kamatala ◽  
Anil Kumar Mardhanpally ◽  
Hemanth Sriram Yel ◽  
Yaku Guguloth ◽  
...  
Keyword(s):  
Aromatic Compounds ◽  
Reaction Times ◽  
Solvent Free ◽  
Microwave Assisted ◽  
Rate Acceleration ◽  
Solvent Free Conditions ◽  
Ultrasonic Assisted

Abstract Silica supported nanogreenacids like Si-KHSO4, and Si-HClO4are explored as reusable catalysts for bromination of aromatic and hetero aromatic compounds using KBr under solvothermal, and solvent-free conditions. Reaction times reduced from Reacions under conventional solvothermal protocols conditions required (4 – 6) hours, while ultrasonic assisted reactions only (9 – 12) minutes for completion. But, solvent-free microwave assisted reactions required only (1-5) minutes exhibiting striking rate acceleration compared to the solvothermal and ultrasonic assisted protocols All the reaction protocols afforded fairly good yields of brominated products, which are comparable with existing protocols.

ZnO@SnO2 Mixed Metal Oxide as an Efficient and Recoverable Nanocatalyst for the Solvent Free Synthesis of Hantzsch 1,4-Dihydropyridines

2019 ◽  
Vol 16 (2) ◽  
pp. 139-144 ◽  
Author(s):  
Bharatkumar M. Sapkal ◽  
Prakash K. Labhane ◽  
Shamrao T. Disale ◽  
Dhananjay H. More
Keyword(s):  
Metal Oxide ◽  
Metal Oxide Nanoparticles ◽  
Reaction Times ◽  
Solvent Free ◽  
Catalyst Loading ◽  
Mixed Metal Oxide ◽  
One Pot ◽  
Mixed Metal ◽  
Solvent Free Conditions ◽  
Three Component Reaction

An efficient synthesis of Hantzsch 1,4-dihydropyridines via a one-pot three-component reaction of ethyl acetoacetate, substituted aldehydes and ammonium acetate in the presence of ZnO@SnO2 mixed metal oxide nanoparticles under solvent-free conditions has been reported. Compare to the reported reactions, this method shows attractive aspects such as cleaner reaction profile, shorter reaction times, minimum catalyst loading and high yields. Isolated catalysts were reused for new reactions without considerable loss of their catalytic activity.

Efficient, microwave-assisted intramolecular 1,3-dipolar cycloadditions of oximes and N-methylnitrones derived from o-alkenylmethoxy-acetophenones

2005 ◽  
Vol 83 (3) ◽  
pp. 260-265 ◽  
Author(s):  
Surinderjit Singh ◽  
M PS Ishar ◽  
Gajendra Singh ◽  
Rajinder Singh
Keyword(s):  
Microwave Irradiation ◽  
Microwave Heating ◽  
Reaction Times ◽  
Solvent Free ◽  
Dipolar Cycloadditions ◽  
Microwave Assisted ◽  
Solvent Free Conditions ◽  
A Minor ◽  
Acetophenone Oxime

Contrary to literature reports, the o-allyloxy- and crotyloxy-acetophenone-oximes (2a, 2b) are transformed to nitrones, which undergo regio- and stereoselective intramolecular 1,3-dipolar cycloadditions, both on microwave heating under solvent free conditions and refluxing in toluene, to afford novel cycloadducts (5a, 5b); the oxazepine-N-oxide (3a) reported to be formed in 98% yield was obtained only as a minor product (~10%). However, o-cinnamyloxy-acetophenone-oxime (2c) under similar conditions undergoes intramolecular N-alkylation to afford nitrone (3c). The reactions carried out under microwave irradiation are cleaner, require shorter reaction times, and have higher yields. Corresponding intramolecular 1,3-dipolar cycloadditions of N-methylnitrones (B), generated in situ from o-alkenylmethoxy-acetophenones (1a–1c) and N-methylhydroxylamine under solvent-free microwave irradiation conditions, are completely regio- and stereoselective, require much shorter reaction times, and afford adducts (4a–4c) in higher yields, as compared with their thermal counterparts.Key words: cycloadditions, nitrones, oximes, o-alkenylmethoxy-acetophenones, microwave, isoxazolidines.

scholarly journals Microwave-assisted synthesis of 2-substituted 4,5,6,7-tetrahydro-1,3-thiazepines from 4-aminobutanol

2020 ◽  
Vol 16 ◽  
pp. 32-38
Author(s):  
María C Mollo ◽  
Natalia B Kilimciler ◽  
Juan A Bisceglia ◽  
Liliana R Orelli
Keyword(s):  
General Procedure ◽  
Reaction Times ◽  
Solvent Free ◽  
Ring Closure ◽  
Microwave Assisted Synthesis ◽  
Microwave Assisted ◽  
Solvent Free Conditions

A general procedure for the synthesis of 2-substituted tetrahydro-1,3-thiazepines by MW-assisted cyclization of 4-thioamidobutanols is presented. The acyclic precursors were prepared in high overall yields by an expeditious three-step diacylation/thionation/deprotection sequence from 4-aminobutanol. Microwave-assisted ring closure of 4-thioamido alcohols promoted by trimethylsilyl polyphosphate (PPSE) in solvent-free conditions allowed for the synthesis of several hitherto unreported seven-membered iminothioethers bearing 2-aryl, alkenyl, aralkyl and alkyl substituents. The cyclodehydration reaction is likely to involve an SN2-type displacement and affords good to excellent yields of the desired heterocycles in very short reaction times.

scholarly journals Solvent-Free Iron(III) Chloride-Catalyzed Direct Amidation of Esters

Molecules ◽  
2020 ◽  
Vol 25 (5) ◽  
pp. 1040
Author(s):  
Blessing D. Mkhonazi ◽  
Malibongwe Shandu ◽  
Ronewa Tshinavhe ◽  
Sandile B. Simelane ◽  
Paseka T. Moshapo
Keyword(s):  
Functional Groups ◽  
Organic Compounds ◽  
Reaction Times ◽  
Solvent Free ◽  
Catalyst Loading ◽  
Free Iron ◽  
Solvent Free Conditions ◽  
Direct Amidation

Amide functional groups are prominent in a broad range of organic compounds with diverse beneficial applications. In this work, we report the synthesis of these functional groups via an iron(iii) chloride-catalyzed direct amidation of esters. The reactions are conducted under solvent-free conditions and found to be compatible with a range of amine and ester substrates generating the desired amides in short reaction times and good to excellent yields at a catalyst loading of 15 mol%.

A Facile and Efficient Conversion of Aldehydes into 1,1-Diacetates (Acylals) using Iron(III) Fluoride as a Novel Catalyst

2007 ◽  
Vol 60 (8) ◽  
pp. 590 ◽  
Author(s):  
V. T. Kamble ◽  
R. A. Tayade ◽  
B. S. Davane ◽  
K. R. Kadam
Keyword(s):  
Large Scale ◽  
Room Temperature ◽  
Reaction Times ◽  
Catalytic Amount ◽  
Solvent Free ◽  
Present System ◽  
Efficient Conversion ◽  
Solvent Free Conditions ◽  
High Yields ◽  
Novel Catalyst

Aldehydes are smoothly converted into the corresponding 1,1-diacetates (acylals) in high yields in the presence of a catalytic amount (0.1 mol-%) of iron(III) fluoride at room temperature. The noteworthy features of the present system are shorter reaction times, chemoselective protection of aldehydes, and solvent-free conditions. The procedure is especially useful for large-scale syntheses as the catalyst is highly effective from the view of activity, selectivity, reusability, and economy in the preparation of 1,1-diacetates (acylals).

scholarly journals Microwave-assisted Synthesis of 2-Substituted 4,5,6,7-Tetrahydro-1,3-thiazepines from 4-Aminobutanol

2019 ◽  
Author(s):  
María C Mollo ◽  
Natalia B Kilimciler ◽  
Juan A Bisceglia ◽  
Liliana R Orelli
Keyword(s):  
General Procedure ◽  
Reaction Times ◽  
Solvent Free ◽  
Ring Closure ◽  
Microwave Assisted Synthesis ◽  
Microwave Assisted ◽  
Solvent Free Conditions

A general procedure for the synthesis of 2-substituted tetrahydro-1,3-thiazepines is presented, by MW-assisted cyclization of 4-thioamidobutanols. The acyclic precursors were prepared in high overall yields by an expeditious three step diacylation/thionation/deprotection sequence from 4-aminobutanol. Microwave assisted ring closure of 4-thioamidoalcohols promoted by trimethylsilyl polyphosphate (PPSE) in solvent-free conditions allowed for the synthesis of several hitherto unreported seven-membered iminothioethers bearing 2-aryl, alkenyl, aralkyl and alkyl substituents. The cyclodehydration reaction is likely to involve a SN2-type displacement and affords good to excellent yields of the desired heterocycles in very short reaction times.

scholarly journals Synthesis of Benzenesulfonamide Derivatives Via Ring Opening of Aziridines In The Presence of Magnetically Retrievable Graphene Based (CoFe@rGO) Nanohybrid.

2021 ◽  
Author(s):  
Ankush Sheoran ◽  
Komal ◽  
Jaspreet Kaur ◽  
Paramdeep Kaur ◽  
Jyoti Agarwal ◽  
...  
Keyword(s):  
Significant Loss ◽  
Solvent Free ◽  
Environmentally Benign ◽  
Nucleophilic Attack ◽  
Catalyst Loading ◽  
Aziridine Ring ◽  
Solvent Free Conditions ◽  
Aryl Amines ◽  
Ft Ir ◽  
Low Catalyst Loading

Abstract Graphene based magnetic nanohybrids have engrossed considerable research curiosity because of their exceptional properties and diverse applications associated with green chemistry. In this regard, a practical, facile and regioselective preparation of 1,2-diamines from N-tosylaziridine/(S)-(+)-2-Benzyl-1-(p-tolylsulfonyl)aziridine and aryl amines in the presence of magnetically separable graphene based nanohybrid (CoFe@rGO) has been proposed under mild and solvent free conditions. The FT-IR, FE-SEM, XRD and EDX spectroscopic analysis confirmed the formation of the CoFe@rGO nanohybrids. For unsymmetrical aziridine, nucleophilic attack of aryl amines was observed to take place selectively at the more substituted carbon atom of aziridine ring. Environmentally benign, efficient, shorter reaction time, solvent-free conditions, low catalyst loading, excellent reaction yields and reusability of the catalyst for six consecutive runs without significant loss in its activity are the key advantages of this protocol.

A simple and eco-sustainable method for the sulfonylation of amines under microwave-assisted solvent-free conditions

RSC Advances ◽  
2014 ◽  
Vol 4 (31) ◽  
pp. 16027-16032 ◽  
Author(s):  
Salah Lakrout ◽  
Hacène K'tir ◽  
Aïcha Amira ◽  
Malika Berredjem ◽  
Nour-Eddine Aouf
Keyword(s):  
Microwave Irradiation ◽  
Reaction Times ◽  
Solvent Free ◽  
Environmentally Benign ◽  
Microwave Assisted ◽  
Catalyst Free ◽  
Solvent Free Conditions

A new environmentally benign, simple, and efficient protocol for the sulfonylation of amines using microwave irradiation under solvent- & catalyst-free conditions is reported. The corresponding sulfonamides were obtained in excellent yields within short reaction times.

Chlorosulfonic Acid Supported Piperidine-4-carboxylic Acid (PPCA) Functionalized Fe3O4 Nanoparticles (Fe3O4-PPCA): The Efficient, Green and Reusable Nanocatalyst for the Synthesis of Pyrazolyl Coumarin Derivatives under Solvent-Free Conditions

2019 ◽  
Vol 22 (2) ◽  
pp. 123-128
Author(s):  
Setareh Habibzadeh ◽  
Hassan Ghasemnejad-Bosra ◽  
Mina Haghdadi ◽  
Soheila Heydari-Parastar
Keyword(s):  
Carboxylic Acid ◽  
Fe3o4 Nanoparticles ◽  
High Efficiency ◽  
Reaction Times ◽  
Chlorosulfonic Acid ◽  
Aromatic Aldehydes ◽  
Solvent Free ◽  
Magnetic Nanocatalyst ◽  
One Pot ◽  
Solvent Free Conditions

Background: In this study, we developed a convenient methodology for the synthesis of coumarin linked to pyrazolines and pyrano [2,3-h] coumarins linked to 3-(1,5-diphenyl-4,5- dihydro-1H-pyrazol-3-yl)-chromen-2-one derivatives using Chlorosulfonic acid supported Piperidine-4-carboxylic acid (PPCA) functionalized Fe3O4 nanoparticles (Fe3O4-PPCA) catalyst. Materials and Methods:: Fe3O4-PPCA was investigated as an efficient and magnetically recoverable Nanocatalyst for the one-pot synthesis of substituted coumarins from the reaction of coumarin with a variety of aromatic aldehydes in high to excellent yield at room temperature under solvent-free conditions. The magnetic nanocatalyst can be easily recovered by applying an external magnet device and reused for at least 10 reaction runs without considerable loss of reactivity. Results and Conclusion: The advantages of this protocol are the use of commercially available materials, simple and an inexpensive procedure, easy separation, and an eco-friendly procedure, and it shows good reaction times, good to high yields, inexpensive and practicability procedure, and high efficiency.

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