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2022 ◽  
Eman M. Sayed ◽  
Reda Hassanien ◽  
Nasser Farhan ◽  
Hanan F. Aly ◽  
Khaled Mahmoud ◽  

Abstract Regioselective cyclocondensation of 2,4-diacetyl-5-hydroxy-5-methyl-3-(3-nitrophenyl/4-nitrophenyl)cyclohexanones 1a,b with cyanothioacetamide afforded the corresponiing 7-acetyl-4-cyano-1,6-dimethyl-6-hydroxy-8-(3-nitrophenyl/4-nitrophenyl)-5,6,7,8-tetrahydro-soquinoline-3(2H)-thiones 2a,b in 93-96% yield. Reaction of compounds 2a,b with some ethyl iodide, 2-chloroacetamide (4a) or its N-aryl derivatives 4b-e by refluxing in ethanol, in the presence of slightly excess molar amounts of sodium acetate trihydrate, for one hour gave 3-ethylthio-5,6,7,8-tetrahydro-isoquinoline 3 and (5,6,7,8-tetrahydroisoquinolin-3-ylthio)acetamides 5a-i, respectively. On heating compounds 5b-d,f,g in ethanol containing a catalytic amount of sodium carbonate, they converted into their isomeric 1-amino- 6,7,8,9-tetrahydrothieno[2,3-c]isoquinoline-2-carboxamides 6b-d,f,g. Structural formulae of all synthesized compounds were characterized on the basis of their elemental analyses and spectroscopic data. Also, the biological evaluation of the synthesized isoquinolines as anticancer and antioxidant agents have been carried out and the obtained results are reported herein.

2022 ◽  
Maryam H. Klidsar ◽  
Marjan Esfahanizadeh ◽  
Pantea Haghverdi ◽  
Salimeh Amidi ◽  
Farzad Kobarfard

Abstract In view of proven antiplatelet activity of hydrazone group containing compounds, two series of hydrazone derivatives were synthesized by coupling appropriate aldehydes with phenyl hydrazine and Isonicotinic acid in the presence of distilled water and a catalytic amount of glacial acetic acid. All synthesized compounds were screened for their antiplatelet activity against induced aggregation by adenosine diphosphate (ADP) and arachidonic acid (AA). The results indicate that compounds in arylhydrazone group had shown satisfactory activity. Among them, 1-(3-methoxybenzylidene)-2-phenylhydrazine (1c), 2-methoxy-4-(2-phenylhydrazono) methyl phenol (1g), and 2-((2-phenylhydrazono) methyl)-1H-pyrrole (1h) were found to be the most potent antiplatelet compounds with IC50 less than 39 μM. Furthermore, the cell toxicity assay, (MTT test) indicates their noncytotoxic in various cell lines. None of the synthesized N-isonicotinohydrazide derivatives in this study excreted sufficient antiplatelet activity.

2022 ◽  
Vol 19 ◽  
Angad B. Barkule ◽  
Yatin U. Gadkari ◽  
Vikas N. Telvekar

Abstract: A rapid and highly efficient methodology for the synthesis of 1, 2, 4-Triazolidine-3-thiones derivatives has been developed in the presence of a catalytic amount of guanidine hydrochloride using water as a solvent. The reaction of thiosemicarbazide with different aryl aldehydes resulted in the formation of title compounds in good yields (85% -95%) with a convenient reaction time (20-30 min). The key advantages of this approach are shorter reaction time, energy efficiency, easy work-up procedure, and wide substrate scope tolerance. Further, the catalyst was recycled without significant loss of its catalytic activity

Renita Manurung ◽  
Muhammad Dedi Anggreawan ◽  
Alwi Gery Agustan Siregar

In this research, the bamboo leaf shows promise as an alternative raw material for silica production. This study investigated the performance of heterogeneous catalyst prepared from silica derived bamboo leaf ash after that impregnated with phosphoric acid at ratio various. The catalyst was characterized by X-Ray Diffraction (XRD), Fourier Transform Infrared Spectroscopy (FTIR), Scanning Electron Microscope Energy Dispersive X-Ray Spectroscopy (SEM-EDS), Brunauer Emmet Teller (BET) and Barrett, Joyner and Halenda (BJH) method and triacetin product analyzed by GC-MS. The optimum condition phosphoric silica catalyst was obtained at phosphoric silica molar ratio of 1:2 and employed in the acetylation of glycerol, respectively. As result, 24 % selectivity for triacetin was obtained in the presence of catalytic amount 5%, molar ratio 1:9 at 100 °C for 4 hours. Bamboo leaf derived phosphoric silica calcined showed high potential to be used as an easy to prepare and high-performance solid catalyst for industrial scale.

2022 ◽  
Vol 34 (2) ◽  
pp. 432-436
Nagamani Rayala ◽  
Sumathi Vodnala ◽  
Supriya Kamsani ◽  
A.K.D. Bhavani ◽  
Nagaraju Myakala ◽  

A novel series of unsymmetrical C-N linked bis heterocycles bearing quinazolinone and acridinedione skeletons have been synthesized in an acid promoted one pot multicomponent reaction. A blend of 6-aminoquinazolin-4-(3H)-one, aromatic aldehydes and cyclohexane-1,3-dione in a simple and efficient condensation-cyclization reaction using hydrochloric acid in catalytic amount as catalyst afforded unsymmetrical bis hybrids in good to excellent yields. Multiheterocyclic hybrid compounds were also synthesized using heterocyclic ring containing aldehyde in three component reaction. The synthesized quinazolinone-acridindione hybrids were characterized using spectroscopic techniques such as a IR, 1H NMR, 13C NMR, ESI-mass and HRMS.

Yuyan Liu ◽  
Xinyi Zhang ◽  
Jiajing Lv ◽  
Chao Zhang ◽  
Xiaotong Chang ◽  

Generation of methylsufonyl-containing thioflavones through a radical relay reaction of methylthiolated phenylalkynones and potassium metabisulfite in the presence of a catalytic amount of sodium methylsulfinate as an initiator under photoinduced...

Catalysts ◽  
2021 ◽  
Vol 12 (1) ◽  
pp. 28
Stefano Serra ◽  
Stefano Marzorati ◽  
Mattia Valentino

In this work, we describe two different biotechnological processes that provide the natural flavour dihydrocoumarin in preparative scale. Both the presented approaches are based on the enzyme-mediated reduction of natural coumarin. The first one is a whole-cell process exploiting the reductive activity of the yeast Kluyveromyces marxianus, a Generally Recognized As Safe (GRAS) microorganism that possesses high resistance to the substrate toxicity. Differently, the second is based on the reduction of natural coumarin by nicotinamide adenine dinucleotide phosphate (NADPH) and using the Old Yellow Enzyme reductase OYE2 as catalyst. NADPH is used in catalytic amount since the co-factor regeneration is warranted employing an enzymatic system based on glucose oxidation, in turn catalysed by a further enzyme, namely glucose dehydrogenase (GDH). Both processes compare favourably over the previously reported industrial method as they work with higher coumarin concentration (up to 3 g/L for the enzymatic process) yet allowing the complete conversion of the substrate. Furthermore, the two approaches have significant differences. The microbial reduction is experimentally simple but the isolated dihydrocoumarin yield does not exceed 60%. On the contrary, the enzymatic approach requires the use of two specially prepared recombinant enzymes, however, it is more efficient, affording the product in 90% of isolated yield.

2021 ◽  
Vol 25 (11) ◽  
pp. 86-92
Sureshkumar K. Dhakhda ◽  
Malay J. Bhatt ◽  
Jyotindra J. Bhatt

A series of 2-(4-phenyl-6-p-tolylpyrimidin-2-ylthio)-N- (4-substituted phenyl)acetamide(4a-o) has been synthesized. Compounds have been characterized and tested for their antioxidant activity. The titled compounds (4a-o) have been synthesized by the reaction between 4-phenyl-6-p-tolylpyrimidine-2-thiol (2) with 2-chloro-N-substituted phenylacetamide (3ao) refluxed in acetone using catalytic amount of K2CO3. Compound (2) has been synthesized from (E)-1-phenyl- 3-p-tolylprop-2-en-1-one (1) with equimolar amount thiourea refluxed in alcoholic KOH to get compound (2). Starting compound chalcone was synthesized by Claisen-Schmidt condensation. All synthesized compounds have been characterized using spectroscopic techniques such as FT-IR, 1H NMR, 13C NMR, Mass Spectrometry and elemental analysis. Antioxidant assay has been performed by using DPPH radical scavenging method. Compounds 4-h and 4-o have shown good antioxidant activity.

2021 ◽  
Vol 6 (40) ◽  
pp. 10739-10745
Xuepu Feng ◽  
Fen Zhao ◽  
Rui Qian ◽  
Mengbi Guo ◽  
Jing Yang ◽  

Nilesh Takale ◽  
Neelakandan Kaliyaperumal ◽  
Gopalakrishnan Mannathusamy ◽  
Rajarajan Govindasamy

Commercially viable manufacturing process for Flecainide Acetate (I) conforming to regulatory specification and cost effective process is reported. Specifically, an improved process for the preparation of Flecainide Acetate allows isolation of anhydrous hydrochloride salt of Compound III, which facilitates the reduction of the pyridine ring with the only catalytic amount of platinum on carbon within 2 hours Therefore, simplifies the synthesis and isolation of Flecainide acetate on a commercial scale to a considerable extent.

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