Reflux In Methanol Research Articles

Sugar derived hydrochar catalysts for enhanced biodiesel production via esterification

Sugars and sugar alcohols are renewable raw materials which can be used for char production. Their acid-catalyzed hydro-carbonization results in the formation of carbon materials with acidic functional groups on the surface, which makes them suitable to be used as heterogeneous catalysts in esterification reactions. Hydrochars materials were prepared by low-temperature slow carbonization of glycerol, xylitol, sucrose, and glucose in the presence of different amounts of H2SO4 (mass ratios from 1 to 4). The hydrochars were extensively characterized and tested in the methanolysis reaction of oleic acid. All the carbon materials were amorphous with features of polyaromatic sheets with hydroxyl (–OH), carboxylic acid (–COOH), and sulfonic (−SO3H) functional groups. The effect of the oleic acid water content on catalytic performance was studied, showing a strong inhibition effect due to the hygroscopic character of catalysts induced by sulfonic groups and other surface groups with oxygen. Under the conditions evaluated (5 % wt. of catalyst, methanol/oleic acid = 9 M ratio, methanol reflux temperature) the sucrose-derived catalyst prepared with the highest H2SO4 content showed the best performance, leading to methyl oleate yield > 90 % after 2 h of reaction, which is only achieved by the majority of analogous catalysts reported in the literature after 4 to 8 h of reaction. The data showed that there is a correlation between the methyl ester yield and the graphitization of the catalyst, as this makes the catalyst more hydrophobic, which is an advantage in esterification catalysts.

Optimization of extraction, separation and purification of baicalin in Scutellaria baicalensis using response surface methodology

Optimizing extraction, separation, and purification processes of bioactive ingredients improves resource utilization and reduces environmental pollution in pharmaceutical industry. Here, we report findings of a study focusing on enhancing baicalin production from Scutellaria baicalensis, an important medicinal crop with increasing market demand. Using response surface methodology, we optimized ultrasonic-assisted extract method (ethanol concentration, ultrasonic temperature, ultrasonic time) for dried powder and decocting method (liquid-solid ratio, decocting time, decocting times) for fresh slices, respectively. Baicalin was separated, purified, and refined through the processing of macroporous resin, alkali-solution, acid precipitating and methanol reflux, respectively, and was quantified via high performance liquid chromatography. The main findings were as follows: (1) Optimal extraction of dried-powder: particle size 80 mesh, liquid-solid ratio 20:1, extraction solvent ethanol 57%, ultrasonic temperature 68°C, ultrasonic time 66 min. (2) Optimal extraction of fresh slices: adding the fresh slices into boiling water, liquid-solid ratio 43:1, decocting for 93 min. (3) Optimal separation: AB-8 macroporous resin, diameter to height ratio 1:15, loading liquid baicalin concentration 25.6 mg/mL, flow rate 1 BV/h, loading volume 8 BV, and elution volume 11 BV. (4) Optimal purification: adjusting the extraction solution pH to 1.0, static placing at 80°C for 12 h, washing the precipitate twice, dissolving the crude baicalin extract with alkali NaOH, and re-precipitating with stronger acid HCl. (5) Optimal refinement: reflux extracting the above baicalin extraction with 75% methanol for 30 min at liquid-solid ratio 15:1. Collectively, these findings provide valuable references for optimizing processing conditions of important medicinal crops in pharmaceutical industry.

In-situ transesterification of microalgae using carbon-based catalyst under pulsed microwave irradiation

In the production of biofuels, microalgae represent an emerging class of renewable feedstock that can address the problems associated with the use of the traditional land-based lignocellulosic biomass. The high lipid content of microalgae makes them ideal in producing fatty acid methyl esters (FAME), the main components of biodiesel. In this study, the transesterification of the lipids in Chlorella vulgaris with methanol was performed in-situ using graphene oxide (GO) under microwave irradiation. From FTIR measurements and titration experiments, GO was shown to possess oxygen functional groups that can serve as catalysts in transesterification. Moreover, the catalytic performance of GO in terms of FAME yield was found to be better than conventional metal-based catalysts. Microwave irradiation, on the other hand, was found to offer a more efficient heating than conventional methods by taking advantage of the excellent microwave absorptivity of methanol and the local heating induced on the surface of GO. Furthermore, irradiation of microwave in pulses rather than in a continuous mode was shown to be more cost-effective. It is proposed that the high energy introduced into the biomass at short time intervals facilitated the release of more lipids by more effectively disrupting the algal cell wall. Lastly, operating with a methanol reflux allowed the microwave-irradiated system to be operated at the boiling point of methanol (Tb = 64.7 °C) while providing a higher FAME yield than an operation at 160 °C without reflux. This study presents graphene oxide under microwave irradiation as a green, carbon-based, and sustainable catalyst in the production of biodiesel from microalgae.

Chemical constituents of the pollen of Typha angustifolia L

Twenty compounds were isolated from the pollen of Typha angustifolia L. using refluxing methanol. These compounds included seven flavonoids (1–7), four glycerolipids (8–11), three alkaloids (12–14), three steroids (15–17), two carboxylic acids (18, 19) and one cerebroside (20). The structures of the compounds were determined by NMR spectroscopy and the spectroscopic data were compared to previously reported data. Compound 17 was isolated from the pollen of T. angustifolia L. for the first time in this study and compounds 8–11 and 16 were discovered in the family Typhaceae for the first time. The chemotaxonomic significance of these compounds isolated from T. angustifolia L. was discussed.

Highly Facile, Regio‐ and Stereoselective Synthesis of Spiropyrrolidine‐5‐aza‐2‐oxindole Derivatives through Multicomponent 1,3‐Dipolar Cycloaddition Reaction and Their In‐Vitro and In‐Silico Biological Studies

AbstractHighly facile one pot synthesis of an assortment of novel spiropyrrolidine 5‐aza‐2‐oxindole derivatives via 1, 3‐di polar cycloaddition reaction has been reported. The underlying concept of Huisgen reaction was applied wherein the azomethine ylides (1,3‐dipoles), generated in‐situ from isatin‐derived compounds and cyclic / acyclic α‐amino acids through the thermal decarboxylation, reacted with exo‐cyclic benzylidine derivatives (dipolarophiles) of 5‐aza‐2‐oxindole afforded plethora of spiropyrrolidine 5‐aza‐2‐oxindoles in excellent yield. High regio‐ and stereo selectivity were accomplished employing this methodology and optimum yield was obtained when reaction carried out under methanol reflux in presence of triethylamine. Furthermore, the compounds were tested for their in‐vitro biological potency as anti‐microbial and anti‐mycobacterial. Antibacterial screening result reveals that out of fifteen compounds four compounds emerged with moderate to reasonable activity against gram negative E. coli and P. aeruginosa. Antifungal screening resulted in identification of two compounds as moderate antifungal agents against A. niger. Antimycobacterial activity results revealed that the four compounds displayed good to moderate in‐vitro activity with MIC=12.5 μg/mL against H37Rv strain as compared to standard pyrazinamide (MIC=3.12 μg/mL). Additionally, molecular docking study was carried out to understand the possible binding modes of the synthesized derivatives within the active site of antibacterial (PDB ID : 3ACX), antifungal (PDB ID : 1IYL) and antimycobacterial (PDB ID : 4TZT) target proteins and were found to display good docking energies. Besides, ADMET properties of the synthesized compounds have shown drug likeness with good oral absorption and moderate BBB permeability.

One-Pot Synthesis of 2-Acetyl-1H-pyrroles from N-Propargylic β-Enaminones via Intermediacy of 1,4-Oxazepines.

A one-pot two-step protocol for the synthesis of 2-acetyl-1H-pyrroles from N-propargylic β-enaminones was described. When treated with zinc chloride in refluxing chloroform, N-propargylic β-enaminones produced in situ 2-methylene-2,3-dihydro-1,4-oxazepines, which, upon further refluxing in methanol with zinc chloride, afforded 2-acetyl-1H-pyrroles. The process was found to be general for a wide variety of N-propargylic β-enaminones and yielded a diverse range of 2-acetyl-1H-pyrroles in good to high yields with large substrate scope and good functional group tolerance. This operationally easy method may provide a rapid access to functionalized 2-acetyl-1H-pyrroles of pharmacological interest.

One-Step conversion of high FFA Crude Karanja oil (Pongamia pinnata) to Bio-diesel Using Portland cement as excellent heterogeneous catalyst

Heterogeneous catalyst was prepared from Portland cement. The prepared heterogeneous catalyst was tested for catalytic activity in the transesterification of non-edible, high free fatty acid feedstock, such as crude karanja oil (CKO), for biodiesel production, at methanol reflux temperature. Gas chromatographic (Gc) analysis technique was used to determine the fatty acid methyl ester yield. The preparation of heterogeneous catalyst from low-cost sources, and the use of non-edible feedstock, only at methanol reflux temperature, were all aimed at reducing the cost of biodiesel production. Insight into the catalytic activities of catalyst was obtained by characterizations for their textural properties, using Brunnear-Emmet-Teller (BET) analysis technique, surface scanning electron microscopy (SEM) and electron dispersive x-ray (EDX) for microstructure, surface morphology and chemical composition; x-ray diffraction (XRD) and Fourier-Transform Infra-Red (FTIR) spectroscopy for structural and functional groups analyses, respectively. Differential thermal and thermogavimetric (DTA/TGA) analyses were performed to determine the proper temperature ranges for the dehydration, decomposition, desorption and oxidation of sample via the TGA curves and their melting points and changes in crystal structures via the DTA curves, for effective determination of calcination temperature. The application of Portland Cement-derived heterogeneous catalyst in the transesterification reaction revealed excellent activity in the transesterification of crude karanja oil, with excellent fatty acid methyl ester yield of over 97.87 %. Operational conditions such as methanol/oil mole ratio (1:3 - 18), catalyst loading (3 - 9 % by wt) and reaction time (0.5 – 7 hours), were investigated to obtain the optimum reaction conditions for the feedstock, while the reaction temperature was kept constant at methanol reflux temperature, to minimise cost of production, in line with the objective of this investigation. Calcined heterogeneous catalysts gave over 80% fatty acid methyl ester yields than the raw counterpart, which were attributed to changes in crystal structures and phases of catalysts, observed in the characterization of catalysts, after calcination. Keywords: Portland cement, heterogeneous catalyst, Crude Karanja oil, transesterification reaction, Feedstock

Michael addition of ethyl anthranilate and phenyl monothioanthranilate to acetylenic esters: experimental and theoretical results

The reaction of ethyl anthranilate with DMAD and with methyl propiolate in dichloromethane in the presence of ethylaluminium dichloride as catalyst at room temperature gives a mixture of the respective E- and Z-intermediate derivatives which do not cyclize even on refluxing for several hours. On carrying out the reaction in refluxing methanol in the absence of the catalyst, only one stereochemical isomer is obtained which is Z-intermediate indicating conversion of less stable isomer into the thermodynamically more stable derivative under these conditions. The resulting product did not cyclize even on refluxing in methanol in the presence of montmorillonite K10 clay catalyst. The reaction of phenyl monothioanthranilate with DMAD and with methyl propiolate gives similar results. A theoretical investigation of the reaction of ethyl anthranilate with methyl propiolate at the B3LYP/6-31 + G(d) level reveals that it occurs in five steps.

Co-processing lard/soybean oil over Ca-based catalysts to greener biodiesel

Fatty Acid Methyl Esters (FAME) were produced from lard/soybean oil (SBO) mixtures using a calcium-based heterogeneous catalyst. The green catalyst was prepared by scallop shell calcination at a relatively low temperature (800 °C) to minimize energy consumption. Images from Scanning Electron Microscopy showed agglomerates of a few tens micrometers with rhombohedral calcite crystallites studded with lime. X-ray diffractogram of fresh catalyst presented overlapped patterns of calcite and lime In tested conditions (methanol reflux temperature, 5% (fat mass basis), methanol/fat = 12 molar ratio, and 150 min), the FAME yield reached 95% (mass) with SBO. However, only 75% FAME yield was obtained from pure lard since the active sites of the catalyst were partially neutralized by lard acidity. Co-processing lard/SBO mixtures attenuated the undesirable fat acidity drawback allowing FAME yields around 90% for mixtures containing less than 50% (mass) of lard. The low-grade fat content of the processed mixture showed no impact on the glycerin quality. Co-processing lard/SBO is a smart strategy to overcome the low-grade fats acidity in biodiesel production process thus providing a more sustainable biodiesel production route.

Reinvestigation of the reaction between aromatic aldehydes, 3-phenyl-5-isoxazolone and sarcosine: Stabilized azomethine ylides as a synthetic equivalent of the methylaminomethyl anion

The reaction of aromatic aldehydes, 3-phenyl-5-isoxazolone and sarcosine proceeds smoothly at reflux in methanol to give (Z)-4-arylidene-3-phenylisoxazol-5(4H)-ones, whereas the addition of isatin to the reaction mixture changes the result, providing oximes of 4-aryl-3-benzoyl-1-methylpyrrolidin-2-ones in 38–72% yield.

High-silica Hβ zeolite catalyzed methanolysis of triglycerides to form fatty acid methyl esters (FAMEs)

Transesterification of biomass-derived triglycerides with methanol (methanolysis of triglycerides) is a promising method for the industrial production of the biodiesel fuel, fatty acid methyl esters (FAMEs). Herein, we present a simple heterogeneous catalytic method for the selective transformation of triglycerides into FAMEs. For the methanolysis of trilaurin under reflux of methanol, a commercially available high-silica Hβ zeolite (Hβ-75, Si/Al = 75) showed a higher yield of methyl laurate than other zeolite catalysts, metal oxides, and conventional heterogeneous and homogeneous catalysts. Under the optimized conditions, the method was widely applicable to the transformation of various triglycerides (C4–C18 frames) into the corresponding FAMEs (yields of 87–93%). The catalyst was furthermore reusable. Quantitative relationships between acidity, hydrophobicity, and reaction rates versus Si/Al ratio of Hβ zeolite catalysts show that a low affinity to glycerol, which arises from the hydrophobicity of the high-silica zeolites, is an important factor for controlling the catalytic activity.

Calcium diglyceroxide as a catalyst for biodiesel production

Calcium diglyceroxide (CaD) was used as the catalyst for biodiesel production through oil methanolysis. It was evaluated its catalytic behavior, its air expo- sure tolerance, and the Ca leaching. CaD catalyst was synthesized from food waste scallop shell derived CaO (obtained by calcination at 900 °C) by contacting with a mixture of equal volumes of glycerin and methanol at 65 °C for 2 h. The CaO obtained by calcination of scallop shell was used as reference catalyst. In standard reaction conditions (2.5 h, methanol reflux temperature, 5 wt% (oil basis) catalyst loading, and methanol:oil = 12:1 moral ratio), CaD presented lower catalytic activity than CaO (FAME yield of 92% against 99%, respectively). 24 h repined CaD presented improved catalytic behavior probably due to the formation of surface Ca −OH groups, achieving 96% of FAME yield. Thermogravimetry (TG) data showed that inorganic residue was larger for biodiesel than for glycerin, being CaD catalyst more soluble than CaO. Data showed that CaD is unstable under reaction conditions, suffering leaching, but the absence of Matter Organic Non-Glycerol (MONG) in the glycerin phase allows to neglect the homogeneous contribution of the leached catalyst. CaD formation during reaction contributes to FAME contamination with Ca and promotes catalyst deactivation thus being an undesired occurrence.

NEW TRANSFORMATIONS OF N -HETARYLCYCLOPENTANO[ d ][1,2,3]TRIAZOLINE RING INTO 5-ALKOXYVALERAMIDINES

It was found that brief refluxing of N -hetarylcyclopentano[ d ][1,2,3]triazolines in methanol resulted in the elimination of nitrogen, accompanied by cyclopentane ring opening with the formation of N -hetarylvaleramidines. Amidines containing pyrimidine-2,4-dione ring were synthesized by a one-step procedure – the reaction of 5-azidopyrimidine-2,4-diones with endocyclic enamines containing a cyclopentene ring proceeded through an N-pyrimidyl-1,2,3-triazoline intermediate. Triazolines containing a 1,3,5-triazine ring at position 1 did not form valeramidines upon refluxing in methanol. N -(1,3,5-triazin-2-yl)cyclopenta[ d ][1,2,3]triazoline containing a morpholine ring at position 6a underwent a different type of transformation upon dissolving in acetic acid, resulting in the formation of N -(1,3,5-triazin-2-yl)diaminoalkene. Mechanisms for these transformations are proposed. Authors: Nikolay A. Belyaev, Tetyana V. Beryozkina, Gert Lubec, Wim Dehaen, Vasiliy A. Bakulev

New transformations of N-hetarylcyclopentano[d][1,2,3]triazoline ring into 5-alkoxyvaleramidines

It was found that brief refluxing of N-hetarylcyclopentano[d][1,2,3]triazolines in methanol resulted in the elimination of nitrogen, accompanied by cyclopentane ring opening with the formation of N-hetarylvaleramidines. Amidines containing pyrimidine-2,4-dione ring were synthesized by a one-step procedure – the reaction of 5-azidopyrimidine-2,4-diones with endocyclic enamines containing a cyclopentene ring proceeded through an N-pyrimidyl-1,2,3-triazoline intermediate. Triazolines containing a 1,3,5-triazine ring at position 1 did not form valeramidines upon refluxing in methanol. N-(1,3,5-triazin-2-yl)cyclopenta[d][1,2,3]triazoline containing a morpholine ring at position 6a underwent a different type of transformation upon dissolving in acetic acid, resulting in the formation of N-(1,3,5-triazin-2-yl)diaminoalkene. Mechanisms for these transformations are proposed.

Design and synthesis of new functionalized isoindigo and (3Z,3′Z)-3,3′-(ethane-1,2-diylidene)bis(indolin-2-one) derivatives

A library of N,N-substituted isoindigo derivatives were prepared by reaction of isoindigo with a variety of alkylating agents in the presence of MeONa under mild conditions in yields of 65–80%. A new, more efficient synthesis of (3Z,3′Z)-3,3′-(ethane-1,2-diylidene)bis(indolin-2-one) is described by reaction of oxindole with glyoxal at reflux in methanol—a small library of N,N′-substituted derivatives were also prepared in 60–70% yield.

High efficiency synthesis of HKUST-1 under mild conditions with high BET surface area and CO2 uptake capacity

This study focuses on the development of a hydrothermal method for the rapid synthesis of good quality copper benzene-1,3,5-tricarboxylate (referred to as HKUST-1) with high yield under mild preparation conditions to address the issues associated with reported methods. Different synthesis conditions and activation methods were studied to understand their influence on the properties of HKUST-1. It was found that mixing the precursors at 50 °C for 3 h followed by activation via methanol refluxing led to the formation of a product with the highest BET specific surface area of 1615 m2/g and a high yield of 84.1%. The XRD and SEM data illustrated that the product was highly crystalline. The sample was also tested on its capacity in CO2 adsorption. The results showed strong correlation between surface area of the sample and its CO2 uptake at 1 bar and 27 °C. The HKUST-1 prepared in this study demonstrated a high CO2 uptake capacity of 4.2 mmol/g. It is therefore concluded that this novel and efficient method can be used in the rapid preparation of HKUST-1 with high surface area and CO2 uptake capacity.

LIGNANS IN OLIVE STONES DISCARDED FROM THE OIL INDUSTRY. COMPARISON OF THREE EXTRACTION METHODS FOLLOWED BY HPLC-DAD-MS/MS AND ANTIOXIDANT CAPACITY DETERMINATION

Lignans are secondary metabolites with diverse chemical structure, and are frequent in food grains. A lignan rich diet have a positive health impact over chronic diseases and protection against certain types of cancer. To enhance the intake of lignans the addition of this compound in processed food could be a solution, so the best approach is to find a source of lignans, especially one that is discarded as waste. In the olive oil production there is a large volume of phytotoxic waste generated, among these is the olive stone (OS), that it is generally burned for fuel. It has been reported the presence of lignans in olive stones extracted with methanol reflux. Three extraction methods for lignans and polyphenolic compounds were assessed: solid-liquid ultrasound assisted extraction with basic hydrolysis, methanolic extraction with Soxhlet, and CO2 supercritical fluid extraction with methanol as a modifier. The determination of lignan content in OS samples were evaluated by HPLC with a core shell C18 column and the detection was in tandem with DAD and MS/MS. The extracts were also evaluated in their antioxidant capacity with ABTS, CUPRAC and ORAC assays and total polyphenol concentration. The aim of this work is to evaluate different methods to extract lignans from OS discarded from the olive oil industry. The main lignan identified in OS extract was pinoresinol. The SFE method to extract pinoresinol was more efficient than Soxhlet and ultrasound assisted solid liquid extractions, producing a higher amount of pinoresinol in the extract in less time and with less amount of co-extracted interferents. The extract produced with Soxhlet had a higher antioxidant capacity.

New asymmetric and symmetric 2-((pyridin-4-yl)methylenamino)-3 aminomaleo nitrile and 2,3-bis((pyridin-4-yl)methylenamino)maleonitrile Schiff bases: Synthesis, experimental characterization along with theoretical studies

Two novel Schiff bases 2-((pyridin-4-yl)methelenamino)-3-aminomaleonitrile (L1) and 2,3-bis((pyridin-yl)methylenamino)maleonitrile (L2) were synthesized by the condensation of 2,3-diaminomaleonitrile and 4-pyridine carboxaldehyde using the reflux in absolute methanol. The light yellow crystalline precipitates of L1 were used for single-crystal X-ray crystallography. Two ligans L1 and L2 were characterized by UV–Vis, FT-IR and 1H/13C NMR spectroscopy. Also the FT-IR, 1H NMR and 13C NMR spectra of the compounds were calculated at the B3LYP/6-31 + G(d) level of theory. The Schiff base L1 with unit cell parameters: a = 19.8380(9), b = 4.7221(2), c = 12.9703(6) Å, V = 1215.02(9) Å3, Z = 4 crystallizes in the orthorhombic crystal system with space group Pna21. The crystal structure was solved by charge flipping using single crystal X-ray diffraction data collected at 120 K. For both ligands, the experimentally obtained NMR and IR spectra were a good agreement with their calculated counterparts.

Magnetic Fe3O4/MCM-41 composite-supported sodium silicate as heterogeneous catalysts for biodiesel production

Abstract This study aims at the development of magnetically recyclable solid catalysts for the production of biodiesel. To achieve this, the magnetically susceptible Fe3O4/MCM-41 composites with core-shell structure were prepared, and sodium silicate was then supported on the magnetic materials by using epichlorohydrin as a cross-linking reagent. The core-shell structured magnetic support and so-prepared solid catalyst were characterized by various techniques. Characterization results showed that the sodium silicate was chemically bridged onto the Fe3O4/MCM-41 composites without obvious damage to the structure of the magnetic support. The solid catalyst exhibited a strong magnetic response and displayed extraordinary catalytic activities in the transesterification of soybean oil for the production of biodiesel, with the oil conversion reaching 99.2% by using the methanol-to-oil molar ratio of 25:1 and catalyst loading of 3 wt% at reflux of methanol after 8 h of reaction. Moreover, the separation of the solid catalyst from reaction mixture was readily achieved by simple magnetic decantation without obvious mass loss, and the solid catalyst could be reused for five times for the heterogeneous transesterification.

Synthesis and Biological Evaluation of 3,4-Dihydro-3-(3-methylisoxazol-5- yl)-2H-benzo[e][1,3]oxazine Derivatives as Anticancer Agents

Background: Cancer is a major health problem worldwide and the major cause of human mortality in the world. The identification of novel structures for effective treatment of cancer is still a major challenge to medicinal chemists. Over the time, important milestones have been achieved in the development of various cancer static drugs for antitumor chemotherapy. Chemotherapy is still highly inadequate, and this necessitates to find novel compounds with potent anticancer activity and minimal or no side effects. Methods: 5-Amino-3-methyisoxazole 1 was treated with different salicylaldehydes 2a-d refluxing in methanol to get the desired products 2-(3-methylisoxazol)-5-ylimino)methyl)phenols 3a-d. The reduction of these imine intermediates with NaBH4 at room temperature produced the amino phenols 4a-d, which underwent smooth ring closure in the presence of formaldehyde, to give isoxazolyl-1,3- benzoxazine derivatives 5a-d. Compound 5d under Suzuki coupling conditions with different aryl and hetero aryl boronic acids furnished the products 7a-d. Results: We synthesized the 3,4-dihydro-8-methoxy-3-(3-methylisoxazol-5-yl)-2H-benzo[e][1,3]oxazine derivatives 5a-5d and 7a-7d from readily accessible starting materials in excellent yields. The newly synthesized compounds 5a-5d and 7a-7d were evaluated for in vitro and potent compounds 5b and 7b were screened for in vivo anticancer activity. Compound 5b has shown potential anticancer activity both in vitro and in vivo. Molecular docking studies were also carried out to balance the experimental results. Conclusion: The structure of all newly synthesized compounds 3-5a-d and 7a-d was confirmed on the basis of IR, 1H NMR, 13C NMR and mass spectral data. Molecular docking studies of compounds 5b and 7b revealed their efficient binding in the hydrophobic pocket in the ATP binding site of EGFR which is consistent with the biological data. Further studies are needed to identify the specific compounds in the series and to develop them as potential anticancer agents. Keywords: Isoxazolyl-1, 3-benzoxazine, Suzuki-Miyura coupling, anticancer activity, Ehrlich Ascites Carcinoma (EAC), Epidermal Growth Factor Receptor (EGFR).