- Design and synthesis of quinoline-pyrimidine inspired hybrids as potential plasmodial inhibitors
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Presently, artemisinin-based combination therapy (ACT) is the first-line therapy of Plasmodium falciparum malaria. With the emergence of malaria parasites that are resistant to ACT, alternative antimalarial therapies are urgently needed. In line with this
- Kayamba, Francis,Malimabe, Teboho,Ademola, Idowu Kehinde,Pooe, Ofentse Jacob,Kushwaha, Narva Deshwar,Mahlalela, Mavela,van Zyl, Robyn L.,Gordon, Michelle,Mudau, Pertunia T.,Zininga, Tawanda,Shonhai, Addmore,Nyamori, Vincent O.,Karpoormath, Rajshekhar
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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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- Synthesis of 4,6-diarylpyrimidin-2(1H)-one derivatives from benzyl halides and (1-bromoethyl)benzene under solvent-free conditions
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A facile synthesis of a series of pyrimidinone derivatives from the reaction of benzyl halides, (1-bromoethyl)benzene and urea in the presence of pyridine N-oxide (PNO) under solvent-free conditions is described. This transformation presumeably occurs via oxidation/cross-aldol condensation/Michael addition/intra molecular cyclization, domino sequence, involving the formation of one C–C bond and two C–N bonds in a single step.
- Beerappa, Mallappa,Shivashankar, Kalegowda
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p. 2150 - 2158
(2018/07/21)
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- Highly effectual synthesis of 4,6-diarylpyrimidin-2(1H)-ones using N,N,N′,N′-Tetramethylethylenediaminium-N,N′-disulfonic acid hydrogen sulfate as a dual-functional catalyst
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The highly effectual synthesis of 4,6-diarylpyrimidin-2(1H)-ones via the one-pot multicomponent reaction of acetophenones with arylaldehydes and urea in the presence of trimethylsilyl chloride and a catalytic amount of the ionic liquid N,N,N′,N′-Tetrameth
- Khanivar, Roghayyeh,Zare, Abdolkarim
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p. 635 - 640
(2018/08/07)
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- Photo-dehydrogenation of 4,6-diaryl-2-oxo-1,2,3,4-tetrahydropyrimidines
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Electron-transfer-induced photo-oxidation of 4,6-diaryl-substituted 2-oxo-1,2,3,4-tetrahydropyrimidines (THPMs) in chloroform under argon atmosphere results in the smooth formation of 4,6-diaryl-substituted 2-oxo-1,2-dihydropyrimidines. Sequentially, elec
- Memarian, Hamid Reza,Sanchooli, Esmael
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p. 1335 - 1346
(2017/06/06)
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- Method for catalytically synthesizing 4,6-diaryl pyrimidine-2(1H)-one derivative by using sulfonic acid functional chitosan
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The invention belongs to the technical field of green organic chemistry, and particularly relates to a method for catalytically synthesizing a pyrimidones derivative by using natural polymer modified sulfonic acid functional chitosan. The method comprises
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Paragraph 0037; 0038; 0058-0062
(2018/01/04)
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- Capto-Dative Stabilization by Thermal Oxidation of 2-Oxo-1,2,3,4-tetrahydropyrimidines
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Various 4,6-diaryl substituted 2-oxo-1,2,3,4-tetrahydropyrimidines (THPMs) were oxidized to 2-oxo-1,2-dihydropyrimidines (DHPMs) by potassium peroxydisulfate (PPS) in aqueous acetonitrile solution under thermal conditions. Based on the proposed oxidation
- Memarian, Hamid R.,Sanchooli, Esmael,Rudbari, Hadi Amiri,Bruno, Giuseppe
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p. 872 - 880
(2016/08/10)
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- Br?nsted acidic ionic liquids catalyzed three-component synthesis of 4,6-diarylpyrimidin-2(1H)-ones under solvent-free conditions
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4,6-Diarylpyrimidin-2(1H)-one derivatives have been synthesized from three-component reaction of aromatic aldehyde derivatives, acetophenone, and urea (thiourea) in the presence of Br?nsted acidic ionic liquids such as triethylammonium hydrogensulfate, N-
- Mollashahi, Ebrahim,Biabangard, Asiyeh
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p. 732 - 738
(2016/01/12)
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- A one-pot three-component synthesis of 4,6-diarylpyrimidin-2(1H)-ones (DAPMs) using atomized sodium in THF under sonic condition
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A simple and an efficient procedure for the synthesis of 4,6-diarylpyrimidin-2(1H)-ones using atomized sodium/THF via a one-pot three-component Biginelli-like cyclocondensation of an aldehyde, a methyl ketone and urea under ultrasonic condition is develop
- Pasha, Mohamed Afzal,Nagashree, Shrivatsa
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p. 1279 - 1283
(2014/04/03)
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- 4,6-Diaryl/heteroarylpyrimidin-2(1H)-ones as a new class of xanthine oxidase inhibitors
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Summary A series of 4,6-diaryl/heteroarylpyrimidones was synthesized employing silica-supported fluoroboric acid under solvent-free conditions in a microwave reactor. The catalytic influence of HBF4-SiO2 was investigated in detail to
- Shukla, Shiwani,Kumar, Dinesh,Ojha, Ritu,Gupta, Manish K.,Nepali, Kunal,Bedi, Preet M. S.
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p. 486 - 495
(2014/07/21)
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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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p. 595 - 599
(2013/07/27)
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- Synthesis of diarylpyrimidinones (DAPMs) using large pore zeolites
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A series of diarylpyrymidin-2(1H)-one (DAPM) belongs to one of the important class of therapeutic and pharmacological active hetrocycles, were synthesized through the multicomponent reactions (MCRs) of aldehydes, ketone and urea, followed by the heterogen
- Mistry, Sunil R.,Maheria, Kalpana C.
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experimental part
p. 210 - 215
(2012/03/09)
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- Iodine-catalyzed versatile synthesis of 4,6-diarylpyrimidin-2(1H)-ones (DAPMs) via one-pot, multicomponent reaction
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An efficient, solvent-free, one-pot, three-component cyclocondensation reaction between aldehyde, ketone, and urea to give 4,6-diarylpyrimidin-2(1H)- ones (DAPMs) using iodine as catalyst is described. This new protocol provides a simple and environmental
- Madhusudana Reddy,Pasha
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experimental part
p. 1875 - 1880
(2011/06/27)
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- H3PMo12O40 catalyzed three-component one-pot synthesis of 4,6-diarylpyrimidin-2(1H)-ones under solvent-free conditions
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4,6-Diarylpyrimidin-2(1H)-one derivatives have been synthesized from three-component one-pot condensation of acetophenone derivatives, aldehydes and urea in the presence of trimethylsilyl chloride and a catalytic amount of H3PMo12Os
- Pourghobadi, Zeinab,Derikvand, Fatemeh
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experimental part
p. 269 - 272
(2010/12/19)
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- H6P2W18O62-18H2O, a green and reusable catalyst for the three-component, one-pot synthesis of 4,6-diarylpyrimidin-2(1H)-ones under solvent-free conditions
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Three-component, one-pot synthesis of 4,6-diarylpyrimidin-2(1H)-ones and 9-phenyl-8-oxa-10,12-diaza-tricyclo[7.3.1.02,7]trideca-2(7),3,5- trien-11-one by condensing acetophenone derivatives, aldehydes, and urea in the presence of trimethylsilyl
- Heravi, Majid M.,Derikvand, Fatemeh,Ranjbar, Leila,Bamoharram, Fatemeh F.
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experimental part
p. 1256 - 1263
(2010/07/05)
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- One-pot synthesis of 4,6-diarylpyrimidin-2(1H)-ones via multi-component reaction promoted by chlorotrimethylsilane
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4,6-Diarylpyrimidin-2(1H)-ones were effectively synthesised by utilising chlorotrimethylsilane (TMSCI) as an efficient promoter in the cyclisation condensation of arylketones, substituted benzaldehydes and urea by a one-pot, threecomponent reaction under
- Wang, Lizhong,Bian, Xiaoqin,Liu, Hui,Sun, Qian,Wang, Cunde
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experimental part
p. 694 - 696
(2011/04/24)
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- Synthesis, fluorescence properties and Zn2+ recognition of 4-Aryl-6-phenylpyrimidin-2(1H)-one
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4-Aryl-6-phenylpyrimidin-2(1H)-ones were synthesised via a three-component one-pot cyclocondensation of aromatic aldehyde, acetophenone and urea catalysed by 0.2 ml (0.024 mol%) of concentration HCI in ionic liquid [BMIM][BF 4]. The fluorescenc
- Wu, Hui,Chen, Xiu-Mei,Wan, Yu,Ye, Ling,Xin, Hai-Qiang,Xu, Hua-Hong,Pang, Li-Ling,Ma, Rui,Yue, Cai-Hui
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experimental part
p. 711 - 714
(2009/09/25)
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- Microwave-expedited one-pot, two-component, solvent-free synthesis of functionalized pyrimidines
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The synthesis of a series of diversely substituted pyrimidines under solvent-free conditions in good yields is described. Under microwave irradiation, a variety of nucleophilic substrates containing the N?C?N unit with ?-dicarbonyl compounds, ethyl cyanoacetate, malononitrile, and chalcones was cyclized to give pyrimidines. A combinatorial type approach for a one-step synthesis has been developed where a ring-closing condensation is followed by spontaneous aromatization to afford 28 functionalized and aryl/alkyl substituted pyrimidines. CSIRO 2007.
- Goswami, Shyamaprosad,Jana, Subrata,Dey, Swapan,Kumar Adak, Avijit
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p. 120 - 123
(2008/02/11)
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- TCT (2,4,6-trichloro-1,3,5-triazine) promoted single-step synthesis of 4,6-diarylpyrimidin-2(1H)-ones under microwave irradiation
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An efficient single-step procedure for the synthesis of 4,6-diarylpyrimidin-2(1H)-ones promoted by Zn(OTf)2-TCT or Bi(OTf)3-TCT under solvent-free microwave irradiation conditions has been developed.{A figure is presented}.
- Khosropour, Ahmad R.,Mohammadpoor-Baltork, Iraj,Khodaei, Mohammad M.,Jokar, Mabubeh
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p. 1551 - 1557
(2007/10/03)
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- Coating compositions stabilized against damage by light, heat and oxygen
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Coatings comprisingA) a binder based on an organic polymer andB) as stabilizer against damage by light, heat and oxygen, a 2-(2′-hydroxyphenyl)-1,3-pyrimidine of the formula I ?in which the radicals R1 to R6 are as defined in claim 1 have an outstanding resistance to the damaging effects of light, oxygen and heat. Compounds of the formula Ib defined in claim 18 are suitable in general for the stabilization of organic material.
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Page column 40
(2008/06/13)
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- Efficient coupling of 2-halopyrimidines to 2,2'-bipyrimidines
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2-chloropyrimidine, 2-chloro- and 2-bromo-4,6-dimethylpyrimidines, 2-chloro- and 2-bromo-4,6-diphenylpyrimidines have been dimerized to the corresponding 2,2'-bipyrimidines in good yields by Tiecco's method using NiCl2, triphenylphosphine and zinc in DMF.
- Nasielski,Standaert,Nasielski-Hinkens
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p. 901 - 906
(2007/10/02)
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- SYNTHESIS AND PROPERTIES OF PHENYL(METHYL)-SUBSTITUTED 2- AND 4-NITROSOPYRIMIDINES
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Phenyl(methyl)-substituted 2- and 4-nitroso- and azoxypyrimidines were synthesized for the first time by the oxidation of phenyl(methyl)-substituted 2- and 4-hydroxyaminopyrimidines by activated MnO2, Ag2CO3 on zeolite, or BaMnO4.Certain chemical properti
- Moskalenko, G. G.,Sedova, V. F.,Mamaev, V. P.
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p. 805 - 811
(2007/10/02)
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- SYNTHESIS OF SUBSTITUTED 2- AND 4-HYDROXYAMINOPYRIMIDINES
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The reaction of 2- and 4-chlorine-containing alkyl(aryl)pyrimidines with hydroxylamine was studied.It was shown that, depending on the amount of hydroxylamine , N,O-dipyrimidinylhydroxyamides or the corresponding 2- and 4-hydroxyaminopyrimidines are formed together with 2- and 4-oxodihydropyrimidines.
- Moskalenko, G. G.,Sedova, V. F..,Mamaev, V. P.
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p. 1232 - 1236
(2007/10/02)
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- Metallation Studies with Pyrimidines
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2-Alkylamino-4,6-diphenylpyrimidines are acylated only at nitrogen after treatment with lithium di-isopropylamide (LDA). 4,6-Diaryl-1-benzylpyrimidin-2(1H)-ones can be acylated and alkylated at the α-CH3 group. 1-Methyl-4,6-di-p-tolylpyrimidin-2(1H)-one f
- Katrizky, Alan R.,Salgado, Hector J.,Chermprapai, Amornsri,Ponkshe, Narayan K.
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p. 153 - 158
(2007/10/02)
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- REACTIVITY OF 4,7-DIHYDRO-5-PHENYL-1,2,4-OXADIAZEPIN-3(2H)-ONES
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The reactions of 4,7-dihydro-5-phenyl-1,2,4-oxadiazepin-3(2H)-ones have been studied.The behaviour of this unsaturated, seven-membered heterocyclic series, which possesses an O-NH-CO-NH functionality, depends on the reagents employed, the experimental con
- Lassalvy, Christiane,Petrus, Clement,Petrus, Francoise
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p. 273 - 278
(2007/10/02)
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