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1.
Rasha S. Gouhar David S. A. Haneen Salwa M. El‐Hallouty 《Journal of heterocyclic chemistry》2019,56(5):1651-1660
A new series of quinazolinone derivatives bearing pyridine, pyrimidine, pyrazole, or pyran moieties were synthesized for the purpose of anticancer cell line evaluation. Synthesis of these derivatives was achieved by the reaction of the ketone 2 with the appropriate aldehydes in the presence of either ethylcyanoacetate or malononitrile and ammonium acetate in one‐pot reaction. Chalcones 6 reacted also with hydrazine hydrate to give the corresponding pyrazolines 7 and reacted with urea or thiourea to give the 2‐oxopyrimidines or the 2‐thioxopyrimidines 8 , respectively. Evaluation of some representative examples of the newly synthesized compounds against cancer cell lines showed promising activity as anticancer agents. 相似文献
2.
Synthesis of New Triazole and Oxadiazole Derivatives of Quinazolin‐4(3H)‐one and Their Antimicrobial Activity 下载免费PDF全文
Kotla Veena Vani Garlapati Ramesh Chunduri Venkata Rao 《Journal of heterocyclic chemistry》2016,53(3):719-726
A series of new triazole derivatives of quinazolin‐4(3H)‐one and new oxadiazole derivatives of quinazolin‐4(3H)‐one were synthesized. The newly synthesized compounds were characterized by IR, 1H NMR, 13C NMR and mass spectral data. All the newly synthesized compounds were screened for antibacterial activity against Staphylococcus aureus, Bacillus subtilis (gram‐positive bacteria), Escherichia coli, Pseudomonas aeruginosa (gram‐negative bacteria), and antifungal activity was carried out against Candida albicans and Aspergillus niger. 相似文献
3.
The title compounds substituted 2‐lactosylthiothieno[2,3‐d]pyrimidin‐4‐ones 6 were synthesized by the glycosyl reaction and alcoholysis reaction of substituted 2‐thioxo‐thieno[2,3‐d]pyrimidin‐4‐ones 4 ,which is formed by the base catalytic and acetic acidify reaction of amino esters 2 with alkyl or arylisothiocyanates and hepta‐O‐acetyl‐lactosyl bromide in good yields. All of the compounds were confirmed by NMR, ESI‐MS, and elemental analysis. 相似文献
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A series of new, 2‐substituted 3‐aryl‐8,9,10,11‐tetrahydro‐5‐methyl[1]benzothieno[3′,2′ : 5,6]pyrido[4,3‐d]pyrimidin‐4(3H)‐ones, compounds 5a – q , were designed and synthesized via the aza‐Wittig reaction as the key step. The iminophosphorane 1 reacted with phenyl isocyanate (or 4‐chlorophenyl isocyanate) to the carbodiimide 4 , which was cyclized to 5 upon addition of different amines, EtOH, or phenols in the presence of a catalytic amount of EtONa or K2CO3 (Schemes 1 and 2). The structures of compounds 5 were confirmed by IR, 1H‐ and 13C‐NMR, EI‐MS, elemental analyses, and, in the case of 5l , by single‐crystal X‐ray diffraction (Figure). 相似文献
6.
Minhang Xin Ying Gao Hua Xiang Dong Chen Yi He Qidong You 《Journal of heterocyclic chemistry》2013,50(1):169-174
A simple and efficient approach to synthesize novel polysubstituted quinazolin‐4(3H)‐ones has been developed, and the key step is a sequential procedure involved iron‐mediated reduction and acid‐catalytic cyclization. The present method provides a convenient and practical strategy for the synthesis of quinazolin‐4(3H)‐one derivatives. 相似文献
7.
A series of new 2‐substituted 3‐(4‐chlorophenyl)‐5,8,9‐trimethylthieno[3′,2′: 5,6]pyrido[4,3‐d]pyrimidin‐4(3H)‐ones 8 were synthesized via an aza‐Wittig reaction. Phosphoranylideneamino derivatives 6a or 6b reacted with 4‐chlorophenyl isocyanate to give carbodiimide derivatives 7a or 7b , respectively, which were further treated with amines or phenols to give compounds 8 in the presence of a catalytic amount of EtONa or K2CO3. The structure of 2‐(4‐chlorophenoxy)‐3‐(4‐chlorophenyl)‐5,8,9‐trimethylthieno[3′,2′: 5,6]pyrido[4,3‐d]pyrimidin‐4(3H)‐one ( 8j ) was comfirmed by X‐ray analysis. 相似文献
8.
The cyclization of aryl ketone anilides 3 with diethyl malonate to affords 4‐hydroxy‐6‐phenyl‐6H‐pyrano[3,2‐c]‐pyridin‐2,5‐diones 4 in good yields. 3‐Acetyl‐4‐hydroxy‐1‐phenylpyridin‐2(1H)‐ones 5 are obtained by ring‐opening reaction of 4‐hydroxy‐6‐phenyl‐6H‐pyrano[3,2‐c]‐pyridin‐2,5‐diones 4 in the presence of 1,2‐diethylene glycol. The reaction of 3‐acetyl‐4‐hydroxy‐1‐phenylpyridin‐2(1H)‐ones 5 with hydroxylamine hydrochloride produces 4‐hydroxy‐3‐[N‐hydroxyethanimidoyl]‐1‐phenylpyridin‐2(1H)‐ones 6 from which 3‐alkyloxyiminoacetyl‐4‐hydroxy‐1‐phenylpyridin‐2(1H)‐ones 7 are obtained by reacting with alkyl bromides or iodides in the presence of anhydrous potassium carbonate with moderate yields. The similar compounds can be synthesized on refluxing 3‐acetyl‐4‐hydroxy‐1‐phenylpyridin‐2(1H)‐ones 5 with substituted hydroxylamine hydrochloride in the presence of sodium bicarbonate with good yields. Most of the synthesized compounds are characterized by IR and NMR spectroscopic methods. 相似文献
9.
We report the efficient preparation of furo[2,3‐d]pyridazin‐4(5H)‐one and its N‐substituted derivatives starting from methyl 2‐methylfuran‐3‐carboxylate. The Me group was converted to the aldehyde group, which was then condensed with hydrazine derivatives. Then, the ester functionalities were hydrolyzed to the corresponding acids, followed by treatment with SOCl2 to give N‐substituted furopyridazinone derivatives. 相似文献
10.
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
11.
Pyrazolone, Isoxazolone, Pyrimidinone, Pyrimidinothione, thiazolidinone and β‐lactam incorporating 2‐oximino benzpyrid‐4‐one derivatives have been synthesized by cyclocondensation addition reaction and cycloaddition of hydrazine hydrate, phenyl hydrazine, hydroxylamine, urea, thiourea, mercapto acetic acid, and chloroacetylchloride, respectively. 相似文献
12.
A new synthesis of 2‐phenylpyrano[3,2‐b]phenothiazin‐4(6H)‐one derivatives was reported. First 2,10‐diacetyl‐3‐hydroxyphenothiazine ( 2 ) was converted into their benzoyloxy esters ( 3a – 3j ) using different aromatic carboxylic acids in the presence of phosphorous oxychloride in pyridine. Benzoyloxy esters were converted into their 1,3‐diones ( 4a – 4j ) by using dry KOH in pyridine via Baker‐Venkataraman transformation reaction. The 1,3‐diones thus obtained were cyclised to pyranophenothiazines ( 5a – 5j ) by refluxing in an acetic acid/HCl mixture. 相似文献
13.
An Efficient Synthesis of 3H‐Pyrrolo[3,2‐d]pyrimidin‐4(5H)‐one Derivatives via an Iminophosphorane 下载免费PDF全文
The iminophosphorane ( 3 ), obtained from reaction of ethyl 3‐amino‐4‐cyano‐1‐phenyl‐1H‐pyrrole‐2‐carboxylate ( 2 ) with triphenylphosphine, hexachloroethane, and triethylamine, reacted with aromatic isocyanates to give carbodiimides ( 4 ). Further reaction of 4 with various amines, phenols, or ROH to give 2,3,5,7‐tetrasubstituted 3H‐pyrrolo[3,2‐d]pyrimidine‐4(5H)‐ones ( 6 ) in satisfactory yields in the presence of catalytic amount of sodium alkoxide or solid potassium carbonate. 相似文献
14.
Fang‐Ming Wang Dan Bao Ming Wang Qing‐Huan Yin Li‐Zhuang Chen Guang‐Fan Han 《Journal of heterocyclic chemistry》2016,53(4):1081-1085
A new series of 3‐(furan‐2‐yl) dibenzo‐diazepin‐1‐one derivatives were synthesized by condensation of 5‐(furan‐2‐yl)‐1,3‐cyclohexanedione, o‐phenylenediamine, and aromatic aldehydes, in which in some of them existed two very close isomer compounds. All the compounds were characterized by IR, MS, 1H NMR, and elemental analysis. Also presented were the crystal structures of 3a , 3b and 3e , which were obtained and determined by X‐ray single‐crystal diffraction. 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
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Ali A. Mohammadi Hamed Rohi Ali Abolhasani Soorki 《Journal of heterocyclic chemistry》2013,50(5):1129-1133
An efficient synthesis of novel 2‐aryl‐3‐(phenylamino)‐2,3‐dihydroquinazolin‐4(1H)‐one derivatives using KAl(SO4)2.12H2O (Alum) as a catalyst from an aldehyde and 2‐amino‐N‐phenylbenzohydrazine in ethanol is described. All synthesized derivatives were screened for anti‐bacterial activity. Some compounds exhibited promising anti‐bacterial activity with reference to standard antibiotics. 相似文献
19.
A direct and efficient method for the preparation of 5‐benzoyldihydro‐2(3H)‐furanones was realized by cyclization of 4‐benzoylbutyric acids in the presence of phenyliodine(III) triflate. 相似文献
20.
R. Sriram R. Sapthagiri L. Ilavarasan A. Ravi 《Journal of heterocyclic chemistry》2017,54(4):2440-2446
Microwave‐assisted efficient one‐pot syntheses of trifluoro substituted 2‐aminobenzimidazole derivative were synthesized using iodoacetic acid mediated cyclodesulfurization of thioureas. This method eliminates need to handle preformed substituted thioureas, requires lesser reaction time and temperature, is facile, and also gives higher yields of the target molecules. 相似文献