- MnO2-MWCNT nanocomposites as efficient catalyst in the synthesis of Biginelli-type compounds under microwave radiation
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A novel Biginelli-like cyclocondensation reaction is efficiently catalyzed by MnO2-CNT nanocomposites as a new catalyst under microwave irradiation and solvent-free conditions in excellent yields. The major advantages of the present method are high yields, short reaction times and solvent-free reaction conditions, reducing reaction steps and purification of products by non-chromatographic methods. The activity, recovery and reusability of the catalyst are found to be good.
- Safari, Javad,Gandomi-Ravandi, Soheila
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- A novel protocol for solvent-free synthesis of 4,6-diaryl-3,4- dihydropyrimidine-2(1H)-ones catalyzed by metal oxide-MWCNTs nanocomposites
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A Biginelli-like condensation is described using acetophenone as active methylene compound with aldehydes and urea to furnish pyrimidinone analogues under solvent-free conditions. In this paper, besides the preparation of nanocomposites based on MWCNTs, o
- Safari, Javad,Gandomi-Ravandi, Soheila
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- PPh3/I2-catalyzed one-pot synthesis of 4,6-diarylpyrimidin-2(1H)-ones
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A method using PPh3/I2-catalyzed three-component Biginelli reaction of aromatic ketone, aromatic aldehyde and urea to synthesize4,6-diarylpyrimidin-2-(1H)-ones is described. Under the experimental conditions, the main reaction produc
- Zhang, Yanzhi,Lei, Min,Xue, Kangsheng,Sun, Guoxiang,Zhou, Yang,Hou, Jinjun,Long, Huali,Zhang, Zijia,Chen, Xubing,Wu, Wanying
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p. 3661 - 3668
(2020/09/11)
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- Structure activity relationship, drug likeness and evaluation of antioxidant activity of some mannich bases of dihydropyrimidinones
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A series of 21 O- and N-Mannich bases of 3,4-dihydropyrimidinones (2a-j and 3a-k) were synthesized by using microwave irradiation technique by multi-component reaction in two steps. All the compounds were evaluated for their free radical scavenging activi
- Mamidala, Ravinder,Bhimathati, Solomon Raj S.,Vema, Aparna
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p. 1767 - 1773
(2019/07/17)
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- Studies on Structural Changes and Catalytic Activity of Y-zeolite Composites of 1,3-disulfoimidazolium trifluoroacetate Ionic Liquid (IL) for Three Component Synthesis of 3,4-dihydropyrimidinones
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Abstract: This report describes the development of six acidic composites of Y-zeolite with 1,3-disulfoimidazolium trifluoroacetate [Dsim][CF3COO] ionic liquid (IL) and displays the gradual increase of acidic IL mediated dealumination within zeo
- Gogoi, Pinky,Dutta, Arup Kumar,Borah, Ruli
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p. 674 - 685
(2017/03/08)
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- Synergistic antifungal effect of cyclized chalcone derivatives and fluconazole against Candida albicans
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The occurrence of invasive fungal diseases, particularly in immunocompromised patients, is life-threatening and increases the economic burden. The rising problem of multi-drug resistance is becoming a major concern for clinicians. In addition, a repertoire of antifungal agents is far less in number than antibacterial drugs. To combat these problems, combination therapy has gained a lot of interest. We previously reported the synergistic interaction of some mono- and bis-dihydropyrimidinone and thione derivatives with fluconazole and amphotericin B for combination antifungal therapy. In this study we used the same approach and synthesized different azole and non-azole derivatives of mono-(M) and bis-(B) chalcones and evaluated their antifungal activity profile alone and in combination with the most commonly used antifungal drug-fluconazole (FLC)-against seven FLC susceptible and three FLC resistant clinically isolated Candida albicans strains. Based on the minimum inhibitory concentration results, the bis-derivatives showed lower MIC values compared to their mono-analogues. Both fractional inhibitory concentration index and isobologram results revealed mostly synergistic, additive or indifferent interactions between the tested compounds and FLC against different Candida isolates. None of the tested compounds showed any effect on energy dependent R6G efflux, revealing that they do not reverse the mechanism of drug efflux. However, surprisingly, these compounds profoundly decreased ergosterol biosynthesis and showed down regulation of ERG11 gene expression, which is the possible mechanism of reversal of azole drug resistance by these compounds. These results provide a platform for further research to develop pyrimidinone/thione ring containing compounds as promising new antifungal agents, which could be used in antifungal combination therapy.
- Ahmad, Aijaz,Wani, Mohmmad Younus,Patel, Mrudula,Sobral, Abilio J.F.N.,Duse, Adriano G.,Aqlan, Faisal Mohammed,Al-Bogami, Abdullah Saad
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p. 2195 - 2207
(2017/12/26)
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- PEG-SANM nanocomposite: A new catalytic application towards clean and highly efficient Biginelli-like reaction under solvent-free conditions
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A series of pyrimidinone derivatives were efficiently synthesized using PEG-SANM nanocomposite as the solid acid nanocatalyst under mild and solvent-free conditions. The generality of the process was successfully demonstrated by variation of the starting
- Dalil Heirati, Seyedeh Zahra,Shirini, Farhad,Shojaei, Abdollah Fallah
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p. 67072 - 67085
(2016/07/30)
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- Organosilane sulfonated graphene oxide in the Biginelli and Biginelli-like reactions
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Organosilane sulfonated graphene oxides (SSi-GO) have been synthesized by a two-step procedure involving the grafting of graphene oxide (GO) using 3-chloropropyltriethoxysilane (CCPTES) and subsequent oxidation using sulfanilic acid. It has been shown tha
- Safari, Javad,Gandomi-Ravandi, Soheila,Ashiri, Samira
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p. 512 - 520
(2016/01/12)
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- Synthesis of Pyrimidinone and 5-unsubstituted 4, 6-diarylpyrimidine-2(1H)-ones by Using Nano Magnetic Catalyst under Solvent Free Condition
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Nano magnetic-supported sulfonic acid is found to be a powerful and reusable heterogeneous catalyst for the efficient synthesis of pyrimidinones. In this study we use various ketones such as acetophenone and cyclopentanone instead of β-keto ester in one-p
- Amoozadeh, Ali,Azhari, Saeede,Kolvari, Eskandar,Otokesh, Somayeh
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p. 968 - 973
(2015/12/01)
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- Green Biginelli-type Reaction: Solvent-free Synthesis of 5-unsubstituted 3,4-dihydropyrimdin-2(1H)-ones
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The Biginelli-type compounds, 5-unsubstituted 3,4-dihydropyrimdin-2(1H)-ones were synthesized by a one-pot three-component condensation of aromatic aldehydes, aromatic ketones and urea in the presence of SnCl4 · 5H2O under solvent-fr
- Wang, Min,Song, Jilei,Lu, Qilin,Wang, Qinglin
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p. 1907 - 1910
(2015/11/09)
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- Fe3O4-CNTs nanocomposites: A novel and excellent catalyst in the synthesis of diarylpyrimidinones using grindstone chemistry
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We investigated the possibility of developing Fe3O 4-CNTs as an efficient and recyclable catalyst for the synthesis of 4,6-diaryl-3,4-dihydropyrimidine-2(1H)-ones under solvent-free conditions via grinding. The procedure is efficient
- Safari, Javad,Gandomi-Ravandi, Soheila
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p. 11486 - 11492
(2014/03/21)
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- 3,4-Hydropyrimidin-2-(1H)one derivatives: Solid silica-based sulfonic acid catalyzed microwave-assisted synthesis and their biological evaluation as antihypertensive and calcium channel blocking agents
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Microwave assisted simple, efficient procedure for one-pot Biginelli condensation reaction of aldehydes, β-ketoesters, and urea or thiourea in solvent-free condition employing solid silica-based sulfonic acid as a novel, heterogeneous reusable catalyst is
- Jetti, Srinivasa Rao,Upadhyaya, Amitbodh,Jain, Shubha
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p. 4356 - 4366
(2015/04/22)
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- Synthesis and in vitro and in vivo antitumor/anticancer activity of novel O-Mannich bases of 4,6-diaryl-3,4-dihydropyrimidine-2(1H)-ones
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A new series of [4,6 substituted diaryl-1,6-dihydropyrimidin-2-yl-oxymethyl]-amines 5a-o have been synthesized by the Mannich condensation on the respective 4,6-diaryl-3,4-dihydropyrimidine-2(1H)-ones 4, in basic medium using formaldehyde along with three
- Venkateshwarlu,Chakradar Rao,Reddy,Narasimha Reddy
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p. 1619 - 1627
(2015/02/18)
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- Synthesis of novel nucleosides and stereoselectivity of N-glycosidation
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An efficient synthetic route for novel nucleosides has been realized. We report the formation of a-isomers in spite of neighboring group participation by the benzoyl group at the 2-position in N-glycosidation as well as discuss the stereoselectivity obser
- Michigami, Kyosuke,Uchida, Satoshi,Adachi, Miho,Hayashi, Masahiko
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supporting information
p. 595 - 599
(2013/07/27)
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- Facile Biginelli-type reactions catalysed by super acidic ionic liquid under solvent-free conditions
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[MeC(OH)2]+ClO4-?as a super acidic ionic liquid is an extremely active catalyst for Biginelli-type reactions. The present method is especially effective for the inactive aliphatic aldehydes. The solvent-free conditions, high catalytic activity, wide substrates tolerance and convenient product isolation make the protocol more advantageous.
- Wang, Liang,Zhou, Min,Chen, Qun,He, Ming-Yang
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p. 712 - 714
(2013/02/23)
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- Synthesis of 3,4-dihydropyrimidin-2(1H)ones and 3,4,5,6,7,8- hexahydroquinazolin-2(1H)-ones via three component cyclocondensation
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3,4 Dihydropyrimidin-2(1H)-ones and 3,4,5,6,7,8-hexahydroquinazolin-2(1H)- ones have been synthesized from the condensation of ketones, aldehydes and urea/thiourea in the presence of sodium tertiary butoxide by the solventless microwave irradiation (MWI)
- Phucho,Nongpiur,Nongrum,Nongkhlaw
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experimental part
p. 346 - 350
(2010/10/03)
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- An efficient synthesis of new 3,4-dihydropyrimidin- 2(1H)-ones incorporating a phenyl moiety at C-5 and C-6 catalyzed by TMSCl and Co(OAc)2.4H2O
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New 3,4-dihydropyrimidin-2-ones having a phenyl moiety at C-5 and C-6 have been prepared by a microwave-assisted Biginelli-like reaction by a three-component, one-pot condensation of an aromatic aldehyde, deoxybenzoin and urea, or thiourea using TMSCl and
- Kefayati, Hassan,Fakhriyannejad, Maryam,Mohammadi, Ali A.
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experimental part
p. 1796 - 1804
(2010/02/28)
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- Three-components condensation catalyzed by molecular iodine for the synthesis of 2,4,6-triarylpyridines and 5-unsubstituted-3,4-dihydropyrimidin- 2(1H)-ones under solvent-free conditions
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One-pot, three-components synthesis of 2,4,6-triarylpyridines and 5-unsubstituted-3,4-dihydropyrimidin-2(1H)-ones was performed under solvent-free conditions using molecular iodine as the catalyst in moderate to good product yields.
- Ren, Yi-Ming,Cai, Chun
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experimental part
p. 49 - 52
(2010/04/06)
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- New three-component cyclocondensation reaction: microwave-assisted one-pot synthesis of 5-unsubstituted-3,4-dihydropyrimidin-2(1H)-ones under solvent-free conditions
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Sixteen 5-unsubstituted-3,4-dihydropyrimidin-2(1H)-ones have been synthesized by microwave-assisted Biginelli reactions in a short and concise manner employing ZnI2 as a catalyst under solvent-free conditions. All products were identified by IR
- Liang, Bing,Wang, Xitian,Wang, Jin-Xian,Du, Zhengyin
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p. 1981 - 1986
(2007/10/03)
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- Aluminium(III) halides mediated synthesis of 5-unsustituted 3,4-dihydropyrimidin-2(1H)-ones via three component Biginelli-like reaction
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5-Unsubstituted-3,4-dihydropyrimidin-2(1H)-ones have been synthesized in excellent yields in a aluminium(III) halides mediated three component cycloaddition of aldehyde, urea and enolizable ketone.
- Saini, Anil,Kumar, Sanjay,Sandhu, Jagir S.
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p. 1690 - 1694
(2008/09/18)
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- AlCl3 mediated three component cyclocondensation for the synthesis of 5-unsubstituted 3,4-dihydropyrimidin-2(1H)-ones
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5-Unsubstituted-3,4-dihydropyrimidin-2(1 H)-ones have been synthesized in excellent yields in aluminium trichloride mediated three component cyclocondensation of aldehyde, urea and enolisable ketones.
- Saini, Anil,Kumar, Sanjay,Sandhu, Jagir S.
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p. 684 - 688
(2007/10/03)
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- Iodotrimethylsilane-accelerated one-pot synthesis of 5-unsubstituted 3,4-dihydropyrimidin-2(1H)-ones: A novel procedure for the Biginelli-like cyclocondensation reaction at room temperature
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A novel Biginelli-like cyclocondensation reaction is efficiently catalyzed by iodotrimethylsilane (Me3SiI) in MeCN. The reaction proceeds at room temperature by a three-component one-pot condensation of ketones with aldehydes and urea to afford
- Sabitha, Gowravaram,Reddy, Kusuma B.,Srinivas, Rangavajjula,Yadav, Jillu S.
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p. 2996 - 2999
(2007/10/03)
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- Novel Biginelli-like three-component cyclocondensation reaction: Efficient synthesis of 5-unsubstituted 3,4-dihydropyrimidin-2(1H)-ones
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Iron (III) catalyzed the three-component Biginelli-like cyclocondensation reaction efficiently in acetonitrile to afford the corresponding 5-unsubstituted 3,4-dihydropyrimidin-2-(1H)-ones in high yields. The first Biginelli-like reactions of urea, aldehyd
- Wang, Zong-Ting,Xu, Li-Wen,Xia, Chun-Gu,Wang, Han-Qing
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p. 7951 - 7953
(2007/10/03)
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- Reaction of α,β-Unsaturated Ketones with Urea. Synthesis and Spectral Properties of 2(1H)-Pyrimidinone Derivatives
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1,3-Diaryl-2-propen-1-ones react with urea to give 4,6-diaryl-3,4-dihydropyrimidinones (IVa-g) that can be further oxidized to the corresponding dehydro analogues (Va-f).The latter compounds are also obtained via interaction of aroylphenylacetylenes with urea.Spectral data, supporting the suggested structures IV and V, are presented.
- Sabri, Salim S.,Hussein, Ahmad Q.,Al-Hajjar, Farouk H.
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p. 512 - 514
(2007/10/02)
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