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1.
Wael S. I. Abou Elmagd 《Journal of heterocyclic chemistry》2011,48(6):1361-1365
3(2‐pyridinylmethylene)‐5‐aryl‐2(3H)‐furanones and 3(3‐pyridinylmethylene)‐5‐aryl‐2(3H)‐furanones were prepared as a mixture of (E) and (Z) stereoisomers by condensing pyridine‐2‐carboxaldehyde and pyridine‐3‐carboxaldehyde with 3‐aroylpropionic acids. The reaction of the furanones 6 and 7 with anhydrous aluminium chloride in benzene led to the formation of 4,4‐diaryl‐1‐(2‐pyridinyl)but‐1,3‐diene ( 8 ) and 4,4‐diaryl‐1‐(3‐pyridinyl)but‐1,3‐diene ( 9 ) as mixtures of geometrical (E,E‐ and E,Z‐) stereoisomers via an intermolecular alkylation mode. When the reaction was carried out in tetrachloroethane as a solvent, the reaction of 6 gave 5‐arylquinoline‐7‐carboxylic acid via intramolecular alkylation mode. This may be considered as a novel method for the synthesis of quinoline derivatives. J. Heterocyclic Chem., (2011). 相似文献
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Design and Synthesis of Novel 3‐(Phenyl)‐2‐(3‐substituted propylthio) Quinazolin‐4‐(3H)‐ones as a New Class of H1‐Antihistaminic Agents 下载免费PDF全文
A series of novel 3‐(phenyl)‐2‐(3‐substituted propylthio) quinazolin‐4‐(3H)‐ones were synthesized by the reaction of 2‐(3‐bromopropylthio)‐3‐(phenyl) quinazolin‐4‐(3H)‐one with various amines. The starting material, 2‐(3‐bromopropylthio)‐3‐(phenyl) quinazolin‐4‐(3H)‐one was synthesized from aniline. When tested for their in vivo H1‐antihistaminic activity on conscious guinea pigs, all the test compounds protected the animals from histamine‐induced bronchospasm significantly. Compound 2‐(3‐(4‐methylpiperazin‐1‐yl) propylthiothio)‐3‐(phenyl) quinazolin‐4(3H)‐one ( Ph5 ) emerged as the most active compound (73.23% protection) of the series when compared with the reference standard chlorpheniramine maleate (70.09% protection). Compound Ph5 shows negligible sedation (5.01 %) compared with chlorpheniramine maleate (29.58%). Therefore, compound Ph5 can serve as the leading molecule for further development into a new class of H1‐antihistaminic agents. 相似文献
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Vakhid A. Mamedov Nataliya A. Zhukova Victor V. Syakaev Tat'yana N. Beschastnova Milyausha S. Kadyrova Anastasiya O. Isaeva Sevil V. Mamedova Elena L. Gavrilova Shamil K. Latypov Oleg G. Sinyashin 《Journal of heterocyclic chemistry》2019,56(8):2221-2234
Facile and efficient methods for the synthesis of 3‐benzylquinoxalin‐2(1H)‐ones and thiazolo[3,4‐a]quinoxalin‐4(5H)‐ones by the reaction of the readily available 3‐(α‐chlorobenzyl)quinoxalin‐2(1H)‐ones and thiourea have been developed, with multiple roles of the latter. Possible mechanisms are discussed. These two‐step sequences can be performed in a one‐pot manner to produce the desired products in moderate to high yields. 相似文献
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Xu‐Hong Yang Ming‐Hu Wu Shao‐Fa Sun Jia‐Li Xie Ming‐Wu Ding Qing‐Hua Xia 《Journal of heterocyclic chemistry》2008,45(5):1365-1369
1‐Aryl‐3‐(2‐ethoxycarbonylphenyl)carbodiimides 2 , obtained from aza‐Wittig reactions of iminophosphorane 1 with aryl isocyanates, reacted with primary diamines in 1:1 and 2:1 molar ratio under mild conditions to give selectively the regioisomers 3‐aminoalkyl‐2‐arylaminoquinazolin‐4(3H)‐ones 3 and 3,3′‐disubstituted bis‐2‐arylaminoquinazolin‐4(3H)‐ones 4 in good yields, respectively. To fully characterize the regioselectivity of aza‐Wittig reactions of 1‐aryl‐3‐(2‐ethoxycarbonylphenyl)carbo‐diimides with primary diamines, crystals of 4e were obtained, and its structure was determined by X‐ray crystallography. 相似文献
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Jorge Trilleras Jairo Quiroga Justo Cobo Christopher Glidewell 《Acta Crystallographica. Section C, Structural Chemistry》2009,65(6):o284-o286
In the title compound, C12H9N3O2S, the thienyl substituent is disordered over two sets of sites with occupancies of 0.749 (3) and 0.251 (3). A combination of N—H...O, C—H...O and C—H...π hydrogen bonds links the molecules into bilayers and these bilayers are themselves linked into a continuous structure by π–π stacking interactions. 相似文献
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The reaction of N,N′‐diarylselenoureas 16 with phenacyl bromide in EtOH under reflux, followed by treatment with NH3, gave N,3‐diaryl‐4‐phenyl‐1,3‐selenazol‐2(3H)‐imines 13 in high yields (Scheme 2). A reaction mechanism via formation of the corresponding Se‐(benzoylmethyl)isoselenoureas 18 and subsequent cyclocondensation is proposed (Scheme 3). The N,N′‐diarylselenoureas 16 were conveniently prepared by the reaction of aryl isoselenocyanates 15 with 4‐substituted anilines. The structures of 13a and 13c were established by X‐ray crystallography. 相似文献
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Yavuz Kysal amil Ik Meri Kksal Hakk Erdgan Nesrin Gokhan 《Acta Crystallographica. Section C, Structural Chemistry》2004,60(4):o232-o234
The title compounds, both C19H20FN3O2, contain essentially planar benzoxazolinone ring systems, within which the C—N bond distances and angles do not differ significantly between the two compounds. In both cases, the piperazine ring adopts an almost perfect chair conformation and the benzoxazolinone ring system lies nearly perpendicular to it. The structures contain intermolecular C—H⋯O contacts, and the interactions between the benzoxazolinone and fluorophenylpiperazine portions of the molecules are segregated. 相似文献
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Shigeru Ohba Yohei Yamamoto Koichi Tanaka 《Acta Crystallographica. Section C, Structural Chemistry》2003,59(7):o370-o372
In the rac isomer of the title compound, C34H28O2, the two C—Phdimethylphenyl bond axes make an angle of 58.7 (1)°. There is no short contact between the two 3,5‐dimethylphenyl rings, although the dihedral angle between them is 4.93 (7)°. The meso isomer has a center of symmetry at the middle of the C=C bond, and the two C—Phdimethylphenyl bond axes are antiparallel to one another. 相似文献
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Hartmut Fuess Michaela Schwarz Erich F. Paulus Jens Hartung Ingrid Svoboda 《Acta Crystallographica. Section C, Structural Chemistry》2006,62(7):o386-o388
The title compound, C20H18ClNOS2, is a thiazole‐derived thiohydroxamic acid O‐ester. The value of Z′ is 3 and the asymmetric unit comprises three molecules of identical helicity along the N—O bond. Two of these show an anti and the third a syn arrangement of substituents attached in positions 3 and 4 to the 1,3‐thiazole nucleus. 相似文献
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Anwar Usman Ibrahim Abdul Razak Hoong‐Kun Fun Suchada Chantrapromma Yan Zhang Jian‐Hua Xu 《Acta Crystallographica. Section C, Structural Chemistry》2002,58(5):o287-o288
In the title compound, C18H13BrClNO3, the heterocyclic ring of the indole is distorted from planarity towards an envelope conformation. The orientations of the indole, oxetane, chloro and bromophenyl substituents are conditioned by the sp3 states of the spiro‐junction and the Cl‐attached C atoms. 相似文献
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Substituted 2‐(benzylamino)‐2H‐1,4‐benzoxazin‐3(4H)‐ones are unstable under alkaline and acidic conditions, undergoing opening of the benzoxazinone ring. 2‐Bromo‐2H‐1,4‐benzoxazin‐3(4H)‐ones show similar degradation under alkaline conditions, while replacement of Br at C(2) to give 2‐hydroxy‐2H‐1,4‐benzoxazin‐3(4H)‐ones was observed only under mild alkaline conditions. Mechanisms of ring opening and degradation to 2‐aminophenol derivatives are proposed. 相似文献
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Anthony J. Burke Helmut W. Schmalle Bernard A. Brady W. Ivo O'Sullivan 《Acta Crystallographica. Section C, Structural Chemistry》2000,56(4):484-486
The title compound, C17H14O4, is an unprecedented new synthetic isoaurone‐type enol ether that has the E configuration. The planar furanone ring is fused to a methoxybenzene ring system, with an interplanar angle of 175.7 (1)°. Due to this ring fusion, the six‐membered ring has a significant amount of ring strain, as shown by the internal ring angle range of 115.8 (1)–124.7 (1)°, whereas the vinylic phenyl ring has internal angles between 119.7 (1) and 120.2 (1)°. The molecules form infinite hydrogen‐bonding layers along the b direction of the form C—H?O, where the keto O atom acts as a bifurcated acceptor. These layers are connected along the c direction by another hydrogen bond with a methoxy H atom as donor. In addition to this connection, the layers are stacked via centres of symmetry by a pair of symmetry‐related benzofuranone ring systems. 相似文献
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Adrenoceptors beta‐3‐subtype mediate lipolysis and in the search for potential beta‐3‐adrenergic receptors agonists for the treatment of obesity, we designed new arylethanolamines (structures 4, 5 ) and aryloxypropanolamines (structures 6, 7 ) derived from 2(3H)‐benzoxazolone and 2(3H)‐benzothiazolone. 相似文献
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Yun Shan Peng Han Sheng Xu Pance Naumov S. Shanmuga Sundara Raj Hoong‐Kun Fun Ibrahim Abdul Razak Seik Weng Ng 《Acta Crystallographica. Section C, Structural Chemistry》2000,56(11):1386-1388
The title compound, C10H9NO2Se, crystallizes as flat molecules linked by selenium–oxygen interactions [Se?O = 3.189 (4) Å] into a linear chain along the a axis of the triclinic cell. The bond dimensions that are derived from ab initio geometry optimization calculations are similar to those determined from the diffraction measurements. 相似文献
16.
Süheyla
zbey Nesrin Gkhan 《Acta Crystallographica. Section C, Structural Chemistry》2004,60(10):o737-o739
A new type of benzothiazolinone derivative with potential pharmacological activity, viz. 6‐(3,4‐difluorobenzoyl)‐3‐[2‐(4‐pyridyl)ethyl]‐1,3‐benzothiazol‐2(3H)‐one, C21H14F2N2O2S, has been prepared and studied by NMR, IR and single‐crystal X‐ray diffraction techniques. The molecule is not planar, the pyridine and difluorobenzene moieties being located above and below the benzothiazole ring system. The carbonyl O atoms are involved in an intramolecular hydrogen‐bond‐type interaction. 相似文献
17.
Raphaël Labruère Philippe Helissey Stéphanie Desbène‐Finck Sylviane Giorgi‐Renault 《Helvetica chimica acta》2013,96(5):919-923
In the context of our aim of discovering new antitumor drugs among synthetic γ‐lactone‐ and γ‐lactam‐fused 1‐methylquinolin‐4(1H)‐ones, we developed a rapid access to 5‐methyl‐1,3‐dioxolo[4,5‐g]furo[3,4‐b]quinoline‐8,9(5H,6H)‐dione ( 9 ) exploiting the γ‐lactone‐fused chloroquinoline 10 previously synthesized in our laboratory (Scheme 1). We also elaborated efficient synthetic methods allowing for a rapid access to two nonclassical bioisosteres of 9 , i.e., a deoxy and a carba analogue. The deoxy analogue 11 was prepared in two steps from the γ‐lactone‐fused quinoline 13 which was also the synthetic precursor of 10 (Scheme 1). The carba analogue 6,9‐dihydro‐5‐methyl‐9‐methylene‐1,3‐dioxolo[4,5‐g]furo[3,4‐b]quinolin‐8(5H)‐one ( 12 ) was easily prepared by HCl elimination from the 9‐(chloromethyl)dioxolofuroquinoline 15 , which was obtained via a three‐component one‐pot reaction from N‐methyl‐3,4‐(methylenedioxy)aniline (=N‐methyl‐1,3‐benzodioxol‐5‐amine; 16 ), commercially available chloroacetaldehyde, and tetronic acid ( 17 ) (Scheme 2). 相似文献
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Victor Marcelo Deflon Karl Eberhard Bessler Martin Kretschmar Ulrich Abram 《无机化学与普通化学杂志》2000,626(7):1545-1549
Tris[3‐hydroxy‐2(1 H)‐pyridinonato] Complexes of Al3+, Cr3+, and Fe3+ – Crystal and Molecular Structures of 3‐Hydroxy‐2(1 H)‐pyridinone and Tris[3‐hydroxy‐2(1 H)‐pyridinonato]chromium(III) Tris[3‐hydroxy‐2(1 H)‐pyridinonato] complexes of Al3+, Cr3+ and Fe3+ are obtained by reactions of 3‐hydroxy‐2(1 H)pyridinone with the hydrates of AlCl3, CrCl3 or Fe(NO3) in aqueous alkaline solutions as polycrystalline precipitates. The compounds are isotypic. X‐ray structure determinations were performed on single crystals of the uncoordinated 3‐hydroxy‐2(1 H)‐pyridinone ( 1 ) (orthorhombic, space group P212121, a = 405.4(1), b = 683.0(1), c = 1770.3(3) pm, Z = 4) and of the chromium compound 3 (rhombohedral with hexagonal setting, space group R3c, a = 978.1(1), c = 2954.0(1) pm, Z = 6). 相似文献
20.
Jií Ludvík Jií Urban Jan Fbry Ivana Císaov 《Acta Crystallographica. Section C, Structural Chemistry》2007,63(4):o259-o262
The title structures, both C10H10N4O, are substitutional isomers. The N—N bond lengths are longer and the C=N bond lengths are shorter by ca 0.025 Å than the respective average values in the C=N—N=C group of asymmetric triazines; the assessed respective bond orders are 1.3 and 1.7. There are N—H⋯O and N—H⋯N hydrogen bonds in both structures, with 4‐amino‐3‐methyl‐6‐phenyl‐1,2,4‐triazin‐5(4H)‐one containing a rare bifurcated N—H⋯N,N hydrogen bond. The structures differ in their molecular stacking and the hydrogen‐bonding patterns. 相似文献