- Synthesis and evaluation of new phenyl acrylamide derivatives as potent non-nucleoside anti-HBV agents
-
As a continuation of our previous work, a series of new phenyl acrylamide derivatives (4Aa-g, 4Ba-t, 5 and 6a-c) were designed and synthesized as non-nucleoside anti-HBV agents. Among them, compound 4Bs could potently inhibit HBV DNA replication in wild-type and lamivudine (3TC)/entecavir resistant HBV mutant strains with IC50 values of 0.19 and 0.18 μM, respectively. Notably, the selective index value of 4Bs was above 526, indicating the favorable safety profile. Interestingly, unlike nucleoside analogue 3TC, 4Bs could significantly inhibit 3.5 kb pgRNA expression. Molecular docking study revealed that 4Bs could fit well into the dimer-dimer interface of HBV core protein by hydrophobic, π–π and H-bond interactions. Considering the potent anti-HBV activity, low toxicity and diverse anti-HBV mechanism from that of nucleoside anti-HBV agent 3TC, compound 4Bs might be a promising lead to develop novel non-nucleoside anti-HBV therapeutic agents, and warranted further investigation.
- Gu, Xiaoke,Zhang, Yinpeng,Zou, Yueting,Li, Xin,Guan, Mingyu,Zhou, Qingqing,Qiu, Jingying
-
-
- Design, Synthesis, and Antimicrobial Activity of Novel Fluorine-Containing Imidazolones
-
Abstract: A simple synthetic protocol have been developed for the preparation of novelN-(4-benzylidene-5-oxo-2-phenyl-4,5-dihydro-1H-imidazol-1-yl)-N′-phenylthiourea derivatives by the reaction of4-benzylidene-2-phenyl-4,5-dihydro-1,3-oxazol-5-ones with N
- Desai,Wadekar,Mehta,Pandit
-
p. 976 - 985
(2021/08/09)
-
- Sulfanilic acid-catalyzed green synthesis of 4-Arylidene-2-phenyl-5(4H)-Oxazolones
-
This study is focused on the catalytic activity of sulfanilic acid (SA) in the straightforward synthesis of 4-Arylidene-2-phenyl-5(4H)-oxazolones via condensation of aromatic aldehydes, hippuric acid, and acetic anhydride under green experimental conditio
- Kiyani, Hamzeh,Aslanpour, Shiva
-
p. 297 - 303
(2018/02/22)
-
- Silica-supported Solvent Approaches More Facile than the Conventional for Erlenmeyer Synthesis with Our Pyridinium Salts
-
The synthesis of pyridinium salts by both conventional/silica-supported muffle furnace and microwave approaches is described. We have optimized the Erlenmeyer synthesis of azalactone with various concentrations of our synthesized pyridinium salts. Among t
- Manikandan, Chitrarasu,Ganesan, Kilivelu
-
p. 929 - 934
(2018/02/19)
-
- An ionic liquid gel: A heterogeneous catalyst for Erlenmeyer-Plochl and Henry reactions
-
An ionic liquid gel has been prepared by entrapping 1-butyl-3-methylimidazolium hydroxide ([Bmim]OH) in an aqueous agar gel. The ionic liquid gel has been characterized by Fourier transform infrared (FT-IR), Fourier transform Raman (FT-Raman) spectroscopy, scanning electron microscopy (SEM), thermogravimetric analysis (TGA) and energy dispersive X-ray analysis (EDX). The ionic liquid gel has been successfully employed as a heterogeneous catalyst in the Erlenmeyer-Plochl reaction involving aldehydes, hippuric acid and acetic anhydride as well as in the Henry reaction between aldehydes and nitromethane in ethanol at room temperature. The heterogeneity of the ionic liquid gel has been confirmed by conducting hot filtration tests and leaching studies. Additionally, the ionic liquid gel could be easily recovered by simple filtration and reused five times without significant loss in catalytic activity.
- Jagadale, Megha,Naikwade, Altafhusen,Salunkhe, Rajashri,Rajmane, Mohan,Rashinkar, Gajanan
-
p. 10993 - 11005
(2018/07/06)
-
- Greener approach: Ionic liquid [Et3NH][HSO4]-catalyzed multicomponent synthesis of 4-arylidene-2-phenyl-5(4H)oxazolones under solvent-free condition
-
We have developed simple, greener, safer multicomponent synthesis series of 4-arylidene-2-phenyl-5(4H) oxazolones 4(a-r) catalyzed by Bronsted acid ionic liquid as triethylammonium hydrogen sulfate [Et3NH][HSO4] and catalytic amount of acetic anhydride and sodium acetate with excellent yields (90–99%). The protocol offers economical, environmentally benign, solvent-free conditions, and recycle–reuse of the catalyst and easily available starting as benzoyl chloride 1, amino acid 2 and a variety of aldehydes 3. The cyclization followed by condensation of benzoyl chloride, amino acid, and a variety of aldehydes catalyzed by ILs [Et3NH][HSO4] and catalytic amount of acetic anhydride and sodium acetate. The final products were confirmed by their characterization data such as FTIR, 1H-NMR, 13C-NMR, Mass, high-resolution mass spectra and were compared with its reported method.
- Jadhav, Santosh A.,Sarkate, Aniket P.,Farooqui, Mazahar,Shinde, Devanand B.
-
p. 1676 - 1683
(2017/09/08)
-
- Synthesis of Erlenmeyer-Pl?chl azlactones promoted by 5-Sulfosalicylic acid
-
5-Sulfosalicylic acid was found as an efficient catalyst in the synthesis of 4-arylidene-2-phenyl-5(4H)-oxazolones by condensation and cyclodehydration of aromatic aldehydes with hippuric acid and acetic anhydride at room temperature. The catalyst was eas
- Kiyani, Hamzeh,Aslanpour, Shiva
-
p. 1314 - 1321
(2017/07/18)
-
- Microwave-assisted efficient synthesis of azlactones using zeolite NaY as a reusable heterogeneous catalyst
-
The efficient preparation of azlactones in the presence of zeolite NaY has been reported. This heterogeneous catalyst was used for efficient synthesis of azlactone derivatives with Ac2O as a condensing agent under microwave irradiation and solvent-free co
- Bodaghifard, Mohammad Ali,Moghanian, Hassan,Mobinikhaledi, Akbar,Esmaeilzadeh, Fatemeh
-
p. 845 - 849
(2017/08/10)
-
- A Facile and Efficient Synthesis of 4-Arylidene-2-phenyl-5(4H)-oxazolones and Their Antimicrobial Evaluation against Selected Human and Phytopathogens
-
A simple and convenient method has been developed for the synthesis of a series of 2-(4-substituted phenyl)-4-(substituted arylidene)-1,3-oxazol-5-ones (5a–j) via reactions of hippuric acid with differently substituted aromatic aldehydes (4a–j) in sodium acetate, potassium acetate, calcium acetate, and ammonium acetate, respectively, which were tested for their efficiency as catalysts in both conventional and microwave-assisted synthetic methods in presence of 4 ? zeolites. The title compounds were evaluated for their antimicrobial properties against selected human pathogens (bacterial and fungal) and phytopathogens (fungal) and were compared with standard drugs. The results of the study are reported.
- Voosala, Christopher,Kilaru, Padma Suhasini,Dasari, Uday Kumar
-
p. 909 - 916
(2016/11/23)
-
- Synthesis and insecticidal evaluation of tetrahydroimidazo[1,2-a]pyridin-5(1H)-one derivatives
-
A series of novel tetrahydroimidazo[1,2-a]pyridine-5(1H)-one derivatives containing a electronegative pharmacophore (=CNO2) were synthesized via practical aza-ene reaction and characterized by 1H NMR, 13C NMR, 19F NMR and HRMS. Preliminary bioassays showed that some of the target compounds exhibited good insecticidal activity against brown planthopper (Nilaparvata lugens) and cowpea aphids (Aphis craccivora) at 500 mg L-1. Among them, compound 11h was active against brown planthopper at 100 mg L-1. The insecticidal activities varied significantly depending on the types and patterns of the substituents, which provided guidance for further investigation on structure modifications.
- Liu, Xuan-Qi,Liu, Ya-Qin,Shao, Xu-Sheng,Xu, Zhi-Ping,Xu, Xiao-Yong,Li, Zhong
-
-
- Microwave-Assisted Erlenmeyer Synthesis of Azlactones Catalyzed by MgO/Al2O3 under Solvent-Free Conditions
-
MgO/Al2O3 catalyzes the synthesis of azlactone derivatives from condensation reaction of aldehydes (or ketones) with hippuric acid and acetic anhydride as a dehydrating agent under microwave irradiation. The low toxicity, low cost, ease of handling, and high activity of MgO/Al2O3 make this procedure particularly attractive. Also, this catalyst can be easily recovered by decant and can be reused for this condensation five times in succession without considerable loss of its catalytic activity.
- Rostamizadeh, Nader,Khajeh-Amiri, Alireza,Moghanian, Hassan
-
p. 631 - 634
(2015/12/26)
-
- An expedient synthesis of oxazolones using a cellulose supported ionic liquid phase catalyst
-
A novel cellulose supported ionic liquid phase catalyst containing hydroxide ions ([CellFemImi]OH) has been synthesized by covalent anchoring of 1-N-ferrocenylmethyl imidazole in the functionalized cellulose matrix followed by an anion metathesis reaction. The [CellFemImi]OH was characterized by various techniques including FT-IR, FT-Raman, 13C solid state NMR, X-ray diffraction, energy dispersive X-ray (EDX) analysis, field emission scanning electron microscopy (FESEM) and thermogravimetric analysis. The [CellFemImi]OH was effectively employed as a heterogeneous catalyst in the synthesis of oxazolones by cyclocondensation of aryl aldehydes with hippuric acid in the presence of acetic anhydride.
- Kurane, Rajanikant,Khanapure, Sharanabasappa,Kale, Dolly,Salunkhe, Rajashri,Rashinkar, Gajanan
-
p. 44135 - 44144
(2016/06/09)
-
- An innovation for development of Erlenmeyer-Pl?chl reaction and synthesis of AT-130 analogous: A new application of continuous-flow method
-
The development of eco-friendly and efficient processes via one-pot multicomponent synthesis is a very attractive topic. In this work, the Erlenmeyer-Pl?chl azlactone synthesis was carried out through unique, safe, fast and practical conditions without any catalyst, applying a simple microreactor and gave the corresponding products exclusively. A continuous, first microflow synthesis of N-benzoylglycine carbamide derivatives as AT-130 analogues catalyzed by Nafion-H@SPIONs was also established successfully.
- Shafiee, Behnaz,Hadian, Laleh,Khosropour, Ahmad R.
-
p. 19861 - 19866
(2016/03/04)
-
- Microwave-assisted efficient and mild synthesis of azlactone derivatives
-
(Formula presented) A convenient and mild procedure for the synthesis of azlactones in the presence of catalytic amounts of calcium hydrogen phosphate as a green, inexpensive and environmentally benign catalyst has been demonstrated. The present protocol is operationally simple and offers some advantages such as good yields, short reaction time, simple work-up, low cost and reusability of catalyst, which makes this method mild and eco-friendly.
- Bodaghifard, Mohammad Ali,Mobinikhaledi, Akbar,Moradi, Khosro
-
p. 193 - 197
(2016/07/15)
-
- A convenient synthesis of 4-arylidene-2-phenyl-5(4H)-oxazolones under solvent-assisted grinding
-
A facile and effective approach for the synthesis of 4-arylidene-2-phenyl-5(4H)-oxazolones has been developed. Under solvent-assisted grinding in the presence of 2,4,6-trichloro-1,3,5-triazine, catalytic triphenylphosphine, and sodium carbonate, dehydrati
- Pattarawarapan, Mookda,Jaita, Subin,Phakhodee, Wong
-
supporting information
p. 3171 - 3174
(2016/07/06)
-
- One flask synthesis of esters of the corresponding 3-substituted 2-benzoylamino acrylic acids using 2-oxazolin-5-ones as synthons
-
A modified route for the fast and facile synthesis of an alkyl 3-substituted 2- benzoylamino acrylate (4) is hereby developed. All the required steps are carried out in the same flask.
- Ahmed, Md. Mizanur,Borthakur, Somadrita,Tripathy, Pradeep K.
-
p. 371 - 372
(2019/01/21)
-
- Synthesis of Erlenmeyer azlactones using arylsulphonyl chloride as cyclocondensing agent
-
A fast and facile procedure for one flask synthesis of (Z)-2-substituted-4- arylmethylene-2-oxazolin-5-ones (3) which are popularly known as Erlenmeyer azlactones, is being reported starting from N-acylglycines (1) and different aromatic aldehydes using arylsulphonyl chloride as cyclocondensing agent in the presence of triethyl amine base and dry benzene. The reaction time is reduced to minute under milder conditions alongwith higher yields of the products.
- Goswami, Limi,Tripathy, Pradeep K.
-
p. 281 - 282
(2019/01/21)
-
- [Et3NH][HSO4]-mediated functionalization of hippuric acid: an unprecedented approach to 4-arylidene-2-phenyl-5(4H)-oxazolones
-
A facile, green and stereoselective approach for the synthesis of azlactones/oxazolones 3(a-q) has been developed. The protocol involves reaction of hippuric acid and substituted heterocyclic/aromatic aldehydes in ionic liquid [Et3NH][HSO4] to yield the desired 4-arylidene-2-phenyl-5(4H)-oxazolones in excellent yields (94-97%) with a high degree of purity. The remarkable feature of this pathway is that the ionic liquid eliminates the use of toxic and expensive acetic anhydride and is endowed with catalytic and medium engineering ability. This eco-friendly approach improved synthetic efficiency (94-97% yield), minimizing the production of chemical waste without using highly toxic reagents for the synthesis and more notably, it promoted the selectivity for Z-azlactones/oxazolones. Density functional theory (DFT) calculations revealed that the Z-isomer of compound 3a is stabilised by 2.32 kcal mol-1 more than the E-isomer. This synthetic scheme possesses diverse applicability and is compatible to a range of functional groups (electron donating/electron withdrawing).
- Parveen, Mehtab,Ahmad, Faheem,Malla, Ali Mohammed,Azaz, Shaista,Silva, Manuela Ramos,Silva, P. S. Pereira
-
p. 52330 - 52346
(2015/06/25)
-
- Nanocrystalline titanium dioxide catalyst for the synthesis of azlactones
-
Titanium dioxide nanoparticles were prepared by a electrochemical reduction method using parameters such as current density, solvent polarity, distance between electrodes, and concentration of stabilizers to control the size of the nanoparticles. The nanoparticles were characterized by UV-Vis spectroscopy, X-ray diffraction, scanning electron microscopy and transmission electron microscopy, and their catalytic performance was tested for the synthesis of a series of 4-aryldiene-2-phenyl-5(4)-oxazolones from the cyclodehydration and condensation of the respective aldehyde, hippuric acid and acetic anhydride. Easy availability, reusability and eco-friendliness were some prominent features of the nanocrystalline titanium dioxide catalyst.
- Anandgaonker, Priyanka,Kulkarni, Ganesh,Gaikwad, Suresh,Rajbhoj, Anjali
-
p. 196 - 200
(2014/03/21)
-
- A concise approach to polysubstituted oxazoles from N-acyl-2-bromo enamides via a copper(i)/amino acid-catalyzed intramolecular C-O bond formation
-
A straightforward and efficient copper(i)/amino acid-catalyzed intramolecular Ullmann-type C-O coupling reaction has been developed. This protocol affords a facile methodology for the synthesis of a series of novel 2,4,5-substituted oxazoles from readily accessible N-acyl-2-bromo enamides under mild conditions. This journal is the Partner Organisations 2014.
- Liu, Bingjie,Zhang, Yueteng,Huang, Gang,Zhang, Xinting,Niu, Pengfei,Wu, Jie,Yu, Wenquan,Chang, Junbiao
-
p. 3912 - 3923
(2014/06/09)
-
- Synthesis, characterization and anticonvulsant activity of substituted imidazolinone derivatives
-
The reaction of glycine with benzoylchloride gave 2-benzamidoacetic acid (1) which on reaction with substituted benzaldehydes in presence of acetic anhydride and anhydrous sodium acetate gave 4-benzylidene-2-phenyloxazol-5(4H)-one derivatives (2a-h). 4-Ni
- Sudha, B. Naga,Subbaiah, N. Yella,Raghavendra,Srikanth,Reddy, C.Venkataramana,Manasa
-
p. 159 - 162
(2019/01/21)
-
- Sonochemical hot-spot assisted one-pot synthesis of 4-arylmethylidene-2- phenyl-4H-oxazol-5-ones using nano-mgo as an efficient catalyst
-
Twelve 4-arylmethylidene-2-phenyl-4H-oxazol-5-ones were prepared in excellent yield by sonicating a mixture of an araldehyde, hippuric acid and acetic anhydride in the presence of a green heterogeneous NanoMgO as a basic catalyst. The catalytic activity o
- Saleh Azzam, Sadeq Hamood,Chandrappa,Pasha, Mohamed Afzal
-
p. 283 - 290
(2013/07/26)
-
- Ammonium metavanadate an efficient catalyst for Erlenmeyer synthesis
-
An efficient method to synthesize azalactone derivatives using ammonium metavanadate (NH4VO3) as catalyst was performed in the absence of solvent. This method is environmentally friendly and affords the product azalactones in high yi
- Madje, Balaji,Ubale, Milind,Bharad, Jagdish,Shingare, Murlidhar
-
p. 1295 - 1299
(2013/01/15)
-
- Microwave-assisted efficient synthesis of azlactone derivatives using TsCl/DMF under solvent-free conditions
-
A simple and efficient procedure for the synthesis of azlactones employing condensation reaction of aromatic aldehydes with hippuric acid has been developed by using the tosyl chloride (TsCl) and dimethylformamide (DMF) system as condensing agent in the absence of solvents under microwave irradiation. The present protocol is operationally simple and offers several advantages such as high yields, short reaction time, and simple workup.
- Moghanian, Hassan,Shabanian, Meisam,Jafari, Hadi
-
experimental part
p. 346 - 349
(2012/06/30)
-
- Novel and chemoselective one-pot synthesis of 4-arylidene-2-phenyl-5(4H)- oxazolones starting from benzyl alcohols promoted by [(C14H 24N4)2W10O32]-[bmim] NO3
-
A new and practical promoter system for one-pot, efficient, chemoselective synthesis of 4-arylidene-2-phenyl-5(4H)-oxazolones using [(C14H 24N4)2W10O32]-[bmim] NO3 under solvent-free conditions is described. The present work opens up a new and ecofriendly synthetic route to Erlenmeyer-Ploechl adducts from primary benzyl alcohols in a one-pot operation. Graphical abstract: [Figure not available: see fulltext.]
- Rostami, Mahboubeh,Khosropour, Ahmad Reza,Mirkhani, Valiollah,Mohammadpoor-Baltork, Iraj,Moghadam, Majid,Tangestaninejad, Shahram
-
experimental part
p. 1175 - 1180
(2012/01/06)
-
- 2W10O32. 2H2O: A novel and powerful catalyst for the synthesis of 4-arylidene-2-phenyl-5(4)-oxazolones under ultrasonic condition
-
Di[1,6-bis(3-methylimidazolium-1-yl)hexane] decatungstate dihydrate ([C6(MIm)2]2W10O32. 2H2O) as a new family of polyoxometalate-based dicationic ionic liquids (POM-DIL) is synthesized and employed as a novel and powerful heterogeneous catalyst in the synthesis of 4-arylidene-2-phenyl-5(4)-oxazolones (azlactones) under ultrasound-assisted solvent-free condition. On the basis of the results, the products were obtained in excellent yields under mild condition. Utilization of easy work-up and purification make it very interesting from an economic perspective. Moreover, a recycling study confirmed that the catalyst can be reused multiple times without significant loss of its activity.
- Rostami, Mahboubeh,Khosropour, Ahmad R.,Mirkhani, Valiollah,Mohammadpoor-Baltork, Iraj,Moghadam, Majid,Tangestaninejad, Shahram
-
experimental part
p. 869 - 877
(2012/04/23)
-
- Organic-inorganic hybrid polyoxometalates: Efficient, heterogeneous and reusable catalysts for solvent-free synthesis of azlactones
-
Two organic-inorganic hybrid polyoxometalates, consist of 1-butyl-3-methylimidazolium salts of (W10O32)4- and (PW12O40)3- polyanions were prepared and characterized by thermal analysis, X-ray diffraction, FT-IR, diffuse reflectance UV-Vis spectroscopic methods and nitrogen absorption-desorption determination (BET). These heterogeneous catalysts were used for synthesis of azlactones by the reaction of aldehydes with hippuric acid and acetic anhydride under solvent-free conditions. These catalysts were reused several times without loss of their activities.
- Rostami, Mahbubeh,Khosropour, Ahmadreza,Mirkhani, Valiollah,Moghadam, Majid,Tangestaninejad, Shahram,Mohammadpoor-Baltork, Iraj
-
experimental part
p. 27 - 34
(2012/01/03)
-
- Catalyzing the Erlenmeyer Pl?chl reaction: organic bases versus sodium acetate
-
An evaluation of organic base versus sodium acetate as the base in the Erlenmeyer Pl?chl reaction was performed. Aldehyde substituents play an important role in these reactions. Organic bases afford fast reactions, but other side reactions were observed. Alternatively, in the presence of solvent, sodium acetate could be used in catalytic amounts rather than the typical stoichiometric quantities. This Letter reports the comparative results for the use of organic bases versus sodium acetate in Erlenmeyer Pl?chl reactions.
- Cleary, Thomas,Rawalpally, Thimma,Kennedy, Nicole,Chavez, Flavio
-
supporting information; experimental part
p. 1533 - 1536
(2010/06/13)
-
- Alum an efficient catalyst for erlenmeyer synthesis
-
A new and efficient method to synthesize azlactone derivatives using alum ascatalyst was performed in the absence of additional solvent. This method is environmentally friendly and affords the product azlactones in high yields after simple workup.
- Madje, Balaji R.,Ubale, Milind B.,Bharad, Jagdish V.,Shingare, Murlidhar S.
-
experimental part
p. 158 - 161
(2012/01/06)
-
- Molecular iodine-catalyzed, mild, effective, ecofriendly, microwave-assisted, one-pot synthesis of 5-arylmethylidene-2-phenyloxazol-4-ones (Azalactones) under solvent-free conditions
-
Fourteen azalactones have been synthesized in excellent yields under solvent-free conditions by heating an aldehyde, hippuric acid, and acetic anhydride in the presence of molecular iodine as a catalyst in a microwave oven. The short reaction time, cleaner reaction, and easy workup make this protocol practical and economically attractive. Copyright
- Reddy, M. B. Madhusudana,Pasha
-
experimental part
p. 1895 - 1898
(2010/09/07)
-
- One-pot process to Z-α-benzoylamino-acrylic acid methyl esters via potassium phosphate-catalyzed Erlenmeyer reaction
-
A practical and efficient two reaction sequence one-pot process for the synthesis of Z-α-benzoylamino-acrylic acid methyl esters was developed. The process involves a potassium phosphate-catalyzed Erlenmeyer reaction of aromatic aldehydes with hippuric acid followed by an oxazolone ring-opening methanolysis. This process afforded a good overall yield and an excellent product quality via a simple workup.
- Cleary, Thomas,Brice, Jodie,Kennedy, Nicole,Chavez, Flavio
-
supporting information; experimental part
p. 625 - 628
(2010/04/05)
-
- Synthesis, characterization and biological activity of 5-arylidene-3-(6,7-dicloro-1,3-benzothiazol-2-yl)-phenyl-3,5-dihydro-4H-imidazol-4-ones
-
Some novel 5-arylidene-3-(6,7-dichloro-1,3-benzothiazol-2-yl)-2-phenyl-3,5-dihydro-4H-imidazol-4-ones (6a-q) have been synthesized and characterized by elemental analyses, IR, NMR, and mass spectra. The products have been evaluated for antibacterial and a
- Baldaniya
-
scheme or table
p. 81 - 84
(2011/01/03)
-
- A new, efficient and chemoselective one-pot protocol for synthesis of 4-arylidene-2-phenyl-5(4H)-oxazolones from aryl aldehyde bisulfite adducts promoted by POCl3
-
(Chemical Equation Presented) A one-pot procedure for the synthesis of 4-arylidene-2-phenyl-5(4H)oxazolones directly from aryl aldehyde bisulfite adducts in the absence of Ac2O in good to excellent yields using phosphoryl chloride is reported. In addition, the observed chemoselectivity can be considered as a noteworthy advantage of this method.
- Khosropour, Ahmad R.,Khodaei, Mohammad M.,Hoseini Jomor, Seyed J.
-
p. 683 - 686
(2008/09/21)
-
- Dodecatungstophosphoric acid (H3PW12O40), samarium and ruthenium (III) chloride catalyzed synthesis of unsaturated 2-phenyl-5(4H)-oxazolone derivatives under solvent-free conditions
-
We have found that dodecatungstophosphoric acid (H3PW 12O40), samarium or ruthenium(III) chloride act as efficient catalysts for the synthesis of unsaturated 2-phenyl-5(4H)oxazolone derivatives under solvent-free condition
- Tikdari, Ahmad Momeni,Fozooni, Samieh,Hamidian, Hooshang
-
experimental part
p. 3246 - 3252
(2009/04/10)
-
- An efficient synthesis of new class of pyrazolo[3,4-b]pyridine-6-one derivatives by a novel cascade reaction
-
(Chemical Equation Presented) A novel cascade reaction of 4-arylidene-2-phenyl-1,3-oxazol-5(4H)-one with 3-methyl-l-phenyl-1H-pyrazol-5- amine was described and a number of new pyrazolo[3,4-b]pyridine-6-one derivatives were synthesized. This new protocol has the advantages of shorter time, higher yields, and lower cost as well as easier operation.
- Shi, Feng,Zhang, Junyong,Tu, Shujiang,Jia, Runhong,Zhang, Yan,Jiang, Bo,Jiang, Hong
-
p. 1013 - 1017
(2008/03/29)
-
- Erlenmeyer synthesis for azlactones catalyzed by ytterbium(III) triflate under solvent-free conditions
-
A series of 4-arylidene-2-phenyl-5(4)-oxazolones were synthesized from cyclodehydration-condensation of hippuric acid, aromatic aldehydes, and acetic anhydride catalyzed by ytterbium(III) triflate under mild conditions in excellent yields. Copyright Taylo
- Yu, Chuanming,Zhou, Baocheng,Su, Weike,Xu, Zhenyuan
-
p. 3447 - 3453
(2007/10/03)
-
- Novel synthesis of unsaturated 5(4H)-oxazolone derivatives with using palladium(II) acetate as a catalyst and microvawe irradiation in solvent-free condition
-
Unsaturated 5(4H)-oxazolones have emerged as an important class of synthons. These compounds have prepared with using palladium(II) acetate under free-solvent conditions with excellent yields and microwave irradiation.
- Hamidian, Hooshang,Tikdari, Ahmad Momeni
-
-
- Montmorillonite K-10 mediated Erlenmeyer synthesis of 4-arylmethylene-2- phenyl-5(4H)-oxazolones
-
Aromatic aldehydes and hippuric acid in acetic anhydride undergoes classical Erlenmeyer synthesis in the presence of a catalytic amount of Montmorillonite K-10 to afford the corresponding azlactones in excellent yields with high selectivity. The azlactone
- Karade,Shirodkar,Dhoot,Waghmare
-
-
- Oxazolone analogs as amyloid aggregation inhibitors and for the treatment of alzheimer's disease and disorders related to amyloidosis
-
Disclosed are compounds of the Formula I and their use in a method of inhibiting the aggregation of amyloid proteins and in a method of imaging amyloid deposits.
- -
-
-
- Calcium acetate catalyzed synthesis of 4-arylidene-2-phenyl-5(4H)- oxazolones under solvent-free conditions
-
Eight 4-arylidene-2-phenyl-5(4H)-oxazolones (azlactones) have been prepared via Erlenmeyer synthesis from aromatic aldehydes and hippuric acid using calcium acetate under solvent-free conditions with microwave irradiation.
- Paul, Satya,Nanda, Puja,Gupta, Rajive,Loupy, André
-
p. 425 - 427
(2007/10/03)
-
- Synthesis and immunomodulatory properties of selected oxazolone derivatives
-
Eleven oxazolone derivatives were synthesized and characterized by 1H NMR, EI, IR and UV spectroscopic and CHN analysis. Three compounds, 4-[(E)-(4-nitrophenyl)methylidene]-2-phenyl-1,3-oxazol-5(4H)-one (11), 4-[(E)-(4-methoxyphenyl)methylidene]-2-methyl-1,3-oxazol-5-one (12) and 4-[(E)-(4-nitrophenyl)methylidene]-2-methyl-1,3-oxazol-5(4H)-one (13) were screened for phagocyte chemiluminescence, neutrophil chemotaxis, T-cell proliferation, cytokine production from mononuclear cells and cytotoxicity. 4-[(E)-(4-Nitrophenyl)methylidene]-2-methyl-1,3-oxazol-5(4H)-one (13) was found to be the most potent immunomodulator in the series.
- Mesaik, Muhammad A.,Rahat, Shagufta,Khan, Khalid M.,Zia-Ullah,Choudhary, Muhammad I.,Murad, Shahnaz,Ismail, Zakiah,Atta-ur-Rahman,Ahmad, Aqeel
-
p. 2049 - 2057
(2007/10/03)
-
- Solid support Erlenmeyer synthesis of azlactones using microwaves
-
A rapid and efficient protocol for the synthesis of azlactones is reported starting from acetyl/benzoylglycine and various aromatic aldehydes in the presence of acetic anhydride and sodium acetate in dry media using silica gel as solid support under microwave irradiation. The mild conditions, excellent yields, high purity. short reaction time and easy work-up are some of the major advantages of this method.
- Mogilaiah,Prashanthi,Reddy, Ch. Srinivas
-
p. 2126 - 2128
(2007/10/03)
-
- Efficient and chemoselective conversion of aryl aldehydes to their azalactones catalysed by Bi(III) salts under solvent free conditions
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Bi(NO3)3.5H2O, Bi(TFA)3 and Bi(OTf)3 were found to be highly powerful and practical catalysts for the synthesis of azalactones under solvent free conditions with excellent yields. In addition, high ch
- Khodaei, Mohammad Mehdi,Khosropour, Ahmad Reza,Jomor, Saied Jabar Hoseini
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p. 638 - 641
(2007/10/03)
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- Bismuth (III) acetate: A new catalyst for preparation of azlactones via the Erlenmeyer synthesis
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Bismuth(III) acetate catalyzes the synthesis of azlactones from aromatic aldehydes in moderate to good yields via the Erlenmeyer synthesis. The relatively low toxicity and low cost of bismuth(III) acetate make this procedure particularly attractive.
- Monk, Keith A.,Sarapa, Dusan,Mohan, Ram S.
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p. 3167 - 3170
(2007/10/03)
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- Synthesis of 2-(2-benzothiazoyl/benzoxazoylthio)-N--5-oxo-2-phenyl/methyl-1H-imidazol-1-yl>acetamides as possible anthelmintics
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Twenty new 2-(2-benzothiazolyl/benzoxazolylthio)-N--5-oxo-2-phenyl/methyl-1H-imidazol-1-yl>acetamides have been synthesised and tested for their anthelmintic activity against H. nana infection in mice.
- Husain, M Imtiaz,Kumar, Vinay
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p. 285 - 288
(2007/10/02)
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- Kinetics and mechanism of aminolysis of (Z)-4-arylidene-2-phenyl-5(4H)oxazolones
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The kinetics of the reactions of a series of (Z)-4-arylidene-2-phenyl-5(4H)oxazolones 1 with n-butylamine and piperidine were studied spectrophotometrically in dioxane, ethanol, and cyclohexane under pseudo-first-order conditions and at different temperat
- Alkaabi, Sharifa S.,Shawali, Ahmad S.
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p. 2515 - 2519
(2007/10/02)
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