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1.
A convenient method was developed for the synthesis of substituted 4-azolyl-1-arylbutanones from the available γ-chlorobutyrophenones
by successive stages of transformation into ketals, alkylation of sodium imidazolate or 1,2,4-triazolate by the ketals in
DMF, and removal of the ketal protection.
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Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 8, pp. 1161–1167, August, 2005. 相似文献
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5-Fluorouracil (5-Fu,1)1 is an important antitumor drug. Some derivatives2,3 have shown better therapeutic efficacy than 5-Fu. In order to find much more better antitumor drugs of its derivatives, several attempts have been made and many different types of its derivatives have been prepared at N1, N3 position4~7. Moreover, several different ways have been used for alkylation of 5-Fu7~10. However, up to now, the arylation of 5-Fu at N1 or N3 position hasn't been reported, and the compound o… 相似文献
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Aromatic nitriles underwent addition of stabase-protected γ-aminopropylmagnesium bromide to afford the corresponding 1-pyrrolines in one step. 相似文献
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HongYU FeiWANG ShouFangZHANG 《中国化学快报》2003,14(6):565-568
In order to search for new potent anti-inflammatory and analgesic agents in pyrrolizinones,the title compounds were designed and synthesized.A series of the compounds were prepared with two different synthetic schemes.Some of the compounds showed remarkable anti-inflammatory and/or analgesic activities on mice. 相似文献
8.
5-Cyanoindazoles are conveniently prepared in two to three steps from commercially available 5-bromo-2-fluorobenzaldehyde. 相似文献
9.
Titanium(IV) chloride-catalyzed addition of diethyl trimethylsilyl phosphite to β-nitrostyrenes affords α-phosphoryl nitronates which, on treatment with low valent titanium in situ generated from titanium(IV) and zinc, are smoothly converted to 1-aryl-1-cyanomethanephosphonates in good yields. 相似文献
10.
Kazuhiro Sugamoto Chiaki Kurogi Yoh-ichi Matsushita Takanao Matsui 《Tetrahedron letters》2008,49(47):6639-6641
Naturally occurring chalcones, namely 4-hydroxyderricin (1), xanthoangelol H (2), deoxyxanthoangelol H (3), and deoxydihydroxanthoangelol H (4), were first synthesized and evaluated for antibacterial activities. 相似文献
11.
B. B. Semenov K. A. Novikov Yu. I. Smushkevich V. N. Azev V. V. Kachala 《Chemistry of Heterocyclic Compounds》2005,41(10):1273-1279
A diastereodirected Pictet-Spengler reaction has been carried out to give the previously unknown 1-aryl(alkyl)-4-phenyl-β-carbolines
and it has been found that all of the β-carbolines diastereomers obtained have predominantly the R*,R*-configuration. The
diastereoselectivity of the given reaction is 44–70%.
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Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 10, pp. 1521–1528, October, 2005. 相似文献
12.
Wei LIU Yuan MA Ying Wu YIN Yu Fen ZHAO 《中国化学快报》2006,17(6):736-738
Anodic cyanation is expected to provide a promising method for synthesis of nitriles by reason of its positional reactivity and simple operation1. Within our ongoing interest in cyano group incorporation into small heterocyclic ring systems2, 3, the elect… 相似文献
13.
Norbert De Kimpe Laurent De Buyck Roland Verhé Freddy Wychuyse Niceas Schamp 《合成通讯》2013,43(7):575-582
Recently1 we described a convenient synthesis of 1-aryl-2, 2-dichloro-1-alkanones 1 by a reaction sequence involving conversion of the parent alkylarylketones into the corresponding N-cyclohexylketimines, followed by chlorination with N-chlorosuccinimide in carbon tetrachloride to afford N-cyclo-hexyl α,α-dichloroketimines, the latter compounds being hydrolyzed in acidic medium to yield the title compounds 1. The relative inaccessibility of compounds of type 1 in the literature was striking. α,α-Dichloroacetophenones 1 (R=H) are 相似文献
14.
水合茚三酮与芳甲基酮、水合肼缩合环化制得2-芳基-3,4-二氮杂芴酮(2); 2经还原得2-芳基-3,4-二氮杂芴(3).2与2-溴联苯格氏试剂反应得到中间体叔醇(4); 4在酸性条件下关环合成了2-芳基-3,4-二氮杂螺二芴,其结构经1H NMR,13C NMR和元素分析表征. 相似文献
15.
Alex F. C. Flores Mauro J. Martins Leandro M. Frigo Pablo Machado Patrick T. Campos Juliana L. Malavolta 《合成通讯》2013,43(5):727-737
Novel 1-aryl-4,4,4-trichloro-1,3-butanediones in good yields (80–97%) were synthesized in one pot through acetal acylation with trichloroacetyl chloride followed by acid hydrolysis. Structures of all compounds were elucidated by elemental analysis, mass spectrometry, and 1H/13C nuclear magnetic resonance (NMR) measurements. The 1H/13C NMR data showed that trichloromethyl-β-diketones 2a–k in solution are predominantly ketoenol. However, the spectroscopic data from 4,4,4-trichloro-2-methyl-1-phenyl-1,3-butabedione (2l) with methyl substituent between carbonyls showed a bias toward the diketo form in solution. X-ray diffraction of monocrystals from 2g and 2i showed that these compounds are cis-ketoenol tautomers. Supplemental materials are available for this article. Go to the publisher's online edition of Synthetic Communcations® to view the free supplemental file. 相似文献
16.
R. S. Baltrushis Z. -I. G. Beresnevichyus I. M. Vizgaitis Yu. V. Gatilov 《Chemistry of Heterocyclic Compounds》1981,17(12):1226-1231
The reaction of aromatic amines with maleic acid or its diethyl ester with subsequent hydrolysis gave N-arylaspartic acids, which were converted to 1-aryl- and 1-aryl-2-thio-5-carboxymethylhydantoins by the action of urea, cyanates, or thiocyanates in an acidic medium. Esterification of the acid products with methanol gave the corresponding carbomethoxymethylhydantoins, which were converted by reduction to tetrahydroimidazole derivatives and by acetylation to acetyl derivatives. Alkylation of the carboxymethylhydantoins with dimethyl sulfate gave 3-methyl derivatives of hydantoins, while alkylation with formaldehyde gave 3-hydroxymethyl derivatives of hydantoins. Data from the x-ray diffraction analysis of 1-phenyl-2-thio-5-carbomethoxymethylhydantoin are presented.Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 12, pp. 1669–1674, December, 1981. 相似文献
17.
The synthesis of 1-(phenylsulfonyl)pyrrole-2-boronic acid has been accomplished by a process involving the directed lithiation of 1-(phenylsulfonyl)-pyrrole. The former has been shown to couple smoothly with aryl bromides and iodides under Suzuki conditions to afford 2-aryl-1-(phenylsulfonyl)pyrroles. 相似文献
18.
Acacetin (4) on reaction with prenyl bromide in the presence of methanolic sodium methoxide yielded 6,8-di-C-prenyl-(5) and 6-C-prenyl-(10) derivatives. The former (5) formed the corresponding bisdihydropyrano derivative (8). Monomethyl derivative of 10 (12) gave monodihydropyrano derivative (13). DDQ reaction of 10 followed by methylation afforded di-O-methyl carpachromene (2); whereas that of 5 gave a mixture of 21 and 22.
Nuclear prenylation of apigenin (3) in a similar way gave 6,8-di-C-C-prenyl-(16), its 7-0-prenyl-(15) and 6-C-prenyl-(18) derivatives. DDQ reaction of 18 provided natural carpachromene.1 The structure of the isopentylated apigenin isolated by Dreyer et al.2 needs further consideration. 相似文献
19.
The aminolysis of 5-aryl-3-arylidene-3H-furan-2-ones by the action of aromatic amines leads to the formation of substituted amides of 4-oxo acids, the subsequent azacyclization of which in the presence of acetic anhydride leads to the formation of 1,5-diaryl-substituted 3-arylidene-3H-pyrrol-2-ones. The mechanism of the occurring and alternative transformations is discussed. 相似文献
20.
The synthesis of optically active acyclic analogues of 3'-azido-3'-deoxythymidine, which lack only the 2'-CH2 of the sugar, is described. The synthesis of some nucleoside analogues that contain the N-acetyl-D-neuraminic acid moiety is also described. 相似文献