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Malose J. Mphahlele Mutshinyalo S. Nwamadi Peace Mabeta 《Journal of heterocyclic chemistry》2006,43(2):255-260
The C‐3 brominated and iodinated derivatives were prepared from the corresponding 2‐arylquinolin‐4(1H)‐ones and their NMe‐4‐oxo derivatives using pyridinium tribromide in acetic acid or iodine‐Na2CO3 mixture in THF. The results of further studies of chemical transformation of the prepared α‐haloenones and preliminary antitumour activity of the 3‐bromo NH‐4‐oxo and NMe‐4‐oxo derivatives are also described. 相似文献
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Anja Siegemund Christine Hartung Sven Baumann Brbel Schulze 《Helvetica chimica acta》2004,87(2):376-381
2‐Aryl‐4,5,6,7‐tetrahydro‐1,2‐benzisothiazol‐3(2H)‐ones 1a – e were synthesized by cyclocondensation of 2‐(thiocyanato)cyclohexene‐1‐carboxanilides 9 as a convenient new method. Their S‐oxides 10 were prepared by two routes, either by oxidation of 1 or dehydration of rac‐cis‐3‐hydroperoxysultims 11 . Furthermore, compounds 1 have been identified by HPLC? API‐MS‐MS as intermediates in the oxidation process of the salts 6 . The hydroperoxides 12b and rac‐trans‐ 11b have been unambiguously detected by HPLC? MS investigations and in the reaction of rac‐cis‐ 13b with H2O2 to the hydroperoxides rac‐trans‐ 11b and rac‐cis‐ 11b . 相似文献
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Petra Marinko Ale Obreza Lucija Peterlin‐Mai
Ale Krbav
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Danijel Kikelj 《Journal of heterocyclic chemistry》2000,37(2):405-409
N‐(2‐Amino‐5,6,7,8‐tetrahydro‐6‐quinazolinyl)acetamide ( 9 ) and N‐(2,4‐diamino‐5,6,7,8‐tetrahydro‐6‐quinazolinyl)acetamide ( 6 ) were synthesized from N‐(4‐oxocyclohexyl)acetamide ( 5 ) as novel peptidomimetic building blocks. With similar purpose, N‐(6‐oxo‐5,6,7,8‐tetrahydro‐2‐quinazolinyl)acetamide ( 18 ) and N‐[2‐(acetylamino)‐6‐oxo‐5,6,7,8‐tetrahydro‐4‐quinazolinyl]acetamide ( 14 ) were prepared from cyclohexane‐1,4‐dione monoethylene ketal ( 11 ). 相似文献
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Milda M. Burbuliene Olegas Bobrovas Povilas Vainilavicius 《Journal of heterocyclic chemistry》2006,43(1):43-47
Treatment of ambident sodium salt of 2‐methylsulfanyl‐4(3H)‐quinazolinone with methyl bromoacetate resulted in N(3)‐alkyl ester formation. Reaction of the resulted ester with hydrazine hydrate gave 2‐methylsulfanyl‐4‐oxo‐3(4H)‐quinazolinyl)acetohydrazide, which underwent intramolecular cyclization under heating in dimethylformamide to give 1‐aminoimidazo[2,1‐b]quinazoline‐2,5(1H,3H)‐dione. The latter took place in acylation reaction and in condensation with aromatic aldehydes. 相似文献
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An Efficient and Facile Synthesis of 5‐(Thiophene‐2‐carbonyl)‐6‐(trifluoromethyl)‐tetrahydro‐pyrimidin‐2(1H)‐one and 6‐(Thiophen‐2‐yl)‐4,5‐dihydropyrimidin‐2(1H)‐one from Same Substrates Under Different Conditions 下载免费PDF全文
Rong Liang‐Ce Yunyun Zha Sheng Xia Linlin Ji Jing Zhang Peijun Cai 《Journal of heterocyclic chemistry》2016,53(1):56-63
A series of 5‐(thiophene‐2‐carbonyl)‐6‐(trifluoromethyl)‐tetrahydropyrimidin‐2(1H)‐one and 6‐(thiophen‐2‐yl)‐4,5‐dihydropyrimidin‐2(1H)‐one derivatives have been synthesized from the reactions of aromatic aldehydes, 4,4,4‐trifluoro‐1‐(thien‐2‐yl)butane‐1,3‐dione and urea under the different conditions with high yields. In this research, it was found that the p‐toluenesulfonic acid was an efficient catalyst for obtaining 5‐(thiophene‐2‐carbonyl)‐6‐(trifluoromethyl)‐tetrahydropyrimidin‐2(1H)‐one derivative. At the same time, solvent‐free and NaOH were the preferred conditions for the synthesis of 6‐(thiophen‐2‐yl)‐4,5‐dihydropyrimidin‐2(1H)‐one derivative. Moreover, because of short reaction time, excellent yields, simple setup, this research offered an efficient process for preparing these kind compounds. 相似文献
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A versatile synthetic method for preparing 4‐hydroxyquinolone and 2‐substituted quinolone compounds from simple benzoic acid derivatives was demonstrated. The synthetic strategies involve the use of well known ethyl acetoacetate synthesis, malonic ester synthesis and reductive cyclization. The key intermediates were keto esters 4a‐e , which could be transformed to 4‐hydroxyquinolones 5a,b or 2‐substituted quinolone ethyl esters 6a‐c depending on the reaction conditions. 4‐Hydroxyquinolone analogues were prepared and investigated for N‐methyl‐D‐aspartate (NMDA) activity in vitro. Among these derivatives, 6,7‐difluoro‐3‐nitro‐4‐hydroxyquinolin‐2(1H)‐one ( 9 ) exhibited moderate activity. 相似文献
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Nam‐Ho You Yasuhiro Nakamura Yasuo Suzuki Tomoya Higashihara Shinji Ando Mitsuru Ueda 《Journal of polymer science. Part A, Polymer chemistry》2009,47(19):4886-4894
A series of aromatic polyimides (PIs) containing pyridazine or pyrimidine in their main chains has been developed. All of the PIs were prepared from newly synthesized diamines, 3,6‐bis(4‐aminophenylenesulfanyl)pyridazine (APP), 4,6‐bis(4‐aminophenylenesulfanyl)pyrimidine (APPM) and aromatic dianhydrides, 4,4′‐[p‐thiobis(phenylenesulfanyl)]diphthalic anhydride (3SDEA) and 4,4′‐oxydiphthalic anhydride (ODPA) via the conventional two‐step polycondensation. The PIs showed good thermal stability with 10% weight loss at temperatures above 450 °C and glass transition temperatures above 190 °C. Films with a 10‐μm thickness exhibited good optical transparency above 80% at 500 nm, high refractive indices ranging from 1.7218 to 1.7499, and low birefringence between 0.0066 and 0.0102. © 2009 Wiley Periodicals, Inc. J Polym Sci Part A: Polym Chem 47: 4886–4984, 2009 相似文献
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Synthesis of Novel Heterocycles Derived from 4‐Arylmethylene‐2‐phenyl‐1,3‐oxazole‐5(4H)‐ones 下载免费PDF全文
Ahmed S. A. Youssef Kamal A. Kandeel Wael S. I. Abou‐Elmagd David S. A. Haneen 《Journal of heterocyclic chemistry》2016,53(3):809-816
The acid hydrazide derivatives 2 were converted into pyrazolone, triazinone, and schiff bases. However, the reaction of Schiff base 12 with malononitrile or thioglycolic acid gives the pyrazolotriazinone or thiazolidinone derivative, respectively. The structures of the newly synthesized compounds were established on the basis of IR, 1H‐NMR, mass spectral data, and elemental analyses. The antimicrobial activities of the synthesized compounds were examined against two types of bacteria and two types of fungi. Some of the tested compounds showed promising activities. 相似文献
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Mulin Zhu Zunting Zhang Dong Xue Jinfeng Qiao Yong Liang Stanislaw F. Wnuk 《中国化学》2013,31(8):1027-1032
A simple method for the cyclocondensation of substituted isoflavones with cyanoacetamide in the presence of sodium hydroxide to give an array of 3‐cyano‐5,6‐diarylpyridin‐2(1H)‐ones in good yields is reported. 相似文献
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Ashraf A. Aly Mohamed Ramadan Ahmed A. M. El‐Reedy 《Journal of heterocyclic chemistry》2019,56(2):642-645
Reaction of four equivalents of 4‐hydroxyquinolin‐2(1H)‐ones with one equivalent of acenaphthoquinone in absolute ethanol, containing catalytic triethylamine, gave 3,3′,3″,3?‐(1,2‐dihydroacenaphthylene)‐1,1,2,2‐tetrayl‐tetrakis(4‐hydroxyquinolin‐2(1H)‐ones) in a good to excellent yields. The structures of the products were elucidated by 1H NMR, 13C NMR, NMR, IR, mass spectra, and elemental analyses. 相似文献
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H. H. Abdel‐Razik 《中国化学会会志》2005,52(1):141-148
Several quinazoline‐2(1H),4(3H)‐dione derivatives were synthesized from pyrimidine‐2(1H),4(3H)‐dione derivative. 相似文献
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《Journal of heterocyclic chemistry》2018,55(1):346-350
In the present investigation, a simple and facile synthesis of a series of 4‐phenylquinoline‐fused pyrrolidin‐2‐ones, namely, 9‐phenyl‐2‐substituted‐2,3‐dihydro‐1H‐pyrrolo[3,4‐b]quinolin‐1‐ones is described, involving the tandem intermolecular C‐N bond formation reaction between readily available ethyl 2‐(chloromethyl)‐4‐phenylquinoline‐3‐carboxylate and various amines followed by in situ intramolecular C–N bond cyclization process in the presence of EtOH‐AcOH (v/v, 10:1) solvent system as the reaction medium. 相似文献
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Jae‐Chul Jung Seikwan Oh Won‐Ki Kim Woo‐Kyu Park Jae Yang Kong Oee‐Sook Park 《Journal of heterocyclic chemistry》2003,40(4):617-623
A variety of 4‐substituted quinolin‐2(1H)‐ones were prepared and evaluated for N‐methyl‐D‐aspar‐tate (NMDA) receptor binding site activity and their abilities to inhibit neurotoxicity. The 4‐(2‐car‐bethoxyethanamino)‐7‐chloro‐3‐nitroquinolin‐2(1H)‐one ( 9b ) exhibited favorable NMDA receptor binding site activity and 7‐chloro‐4‐(benzylamino)‐3‐nitroquinolin‐2(1H)‐one ( 9c ) showed the most potent neurotoxicity among them. The synthetic strategies involve the use of well known keto ester condensation and reductive ring cyclization of intermediates ( 2a‐d ) to afford 4‐substituted quinolin‐2(1H)‐ones. 相似文献
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Synthesis of novel 4-(4-methylsulfonylphenyl)-3-phenyl-2(3H)-thiazole thione derivatives with functionalized diarylheterocycle pharmacophore as potential COX-2 inhibitors was described. The title compounds were synthesized by cyclocondensation of corresponding dithiocarbamate and 2-bromo-1-(4-methylsulfonylphenyl)ethanone, followed by dehydration with H2SO4. All of the target compounds were characterized by ^1H NMR, IR and mass spectral data. 相似文献