共查询到20条相似文献,搜索用时 109 毫秒
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1,3-二苯基-2-吡唑啉-5-酮(1)对查而酮(苯丙烯酰苯,2)的碱性催化加成,生成相应的Michael加成物,4-[α-(苯甲酰甲基)苄基]-1,3-二苯基-2-吡唑啉-5-酮(3),3在沸醇中经肼或羟胺处理得腙或肟(4),4经沸乙酸处理生成1和2的吡唑啉衍生物(5)的混合物,3的还原产物为相应的仲醇(6a~c).Grignard试剂与3反应生成叔醇(6d~1),新化合物的结构经元素分析,IR,~1H和~(13)C NMR证明。 相似文献
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吡唑类衍生物是一类具有很好生物活性的化合物,具有很高除草或杀虫活性的吡唑类化合物文献中已有大量的报导[1]。因此研究其合成方法显得很重要。我们最初希望通过5-氨基-3-苄硫基-4-乙氧羰基吡唑经重氮化反应去氨基制备3-苄硫基-4-乙氧羰基吡唑,然后继续衍生化合成系列吡唑类化合物。 相似文献
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Seiko Nan'ya Etur Maekawa Hitoshi Hayakawa Yukio Kitaguchi Yoshio Ueno 《Journal of heterocyclic chemistry》1985,22(6):1483-1485
The 5H-pyrido[2,3-a]phenoxazin-5-one derivatives and 5H-pyrido[3,2-a]phenoxazin-5-one derivatives were prepared by the condensation of substituted 2-aminophenols with 6,7-dibromo-5,8-quinolinequinone followed by dehalogenation in the presence of sodium hydrosulfite dissolved in aqueous pyridine under a nitrogen atmosphere. 相似文献
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A. N. Grinev A. K. Chizhov V. I. Shvedov T. F. Vlasova 《Chemistry of Heterocyclic Compounds》1974,10(2):193-196
In the reaction of o-nitrobenzenesulfenyl chloride with 5-hydroxyindole derivatives, electrophilic substitution occurs in the 3 position. When there is a carbethoxy group in the 3 position, the o-nitrobenzenesulfenyl residue enters the 6 position. The corresponding 5-hydroxy derivatives, the aminomethylation of which leads to 4-dimethylaminomethyl derivatives, were obtained by hydrolysis of the 5-acetoxy derivatives of o-nitrophenyl 3-indolyl sulfides. 相似文献
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Various procedures for converting 5-fluorouracil into its methyl, butyl and hexyl derivatives are described. Structures were established as the N,N'-dialkyl derivatives using mass spectrometry or combined gas-liquid chromatography-mass spectrometry. The reaction conditions, i.e., the amount of derivatization reagents and reaction time, were optimized. Gas-liquid chromatographic characteristics of the derivatives were investigated on different stationary liquid phases, and 2% or 3% SP-2250, 5% XE-60 and 5% OV-1 were found to be superior. With 5-chlorouracil as the internal standard a linear response for the various derivatives was observed in the microgram range. The applicability of the different dialkyl derivatives in the measurement of 5-fluorouracil in biological materials is discussed. 相似文献
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As an antitumor drug, because of its low efficacy and high toxicity, several modifications have been made on 5-fluorouracil (5-Fu). Some compounds have been found to be highly efficient and much less toxic for the treatment of various solid tumors1~4. Among them, deoxyfluridine (Furtulon) has been used clinically for several years. In our previous work, we have prepared several substituted derivatives of 5-Fu and the primary result shows that some of them have certain antitumor activity5,6. … 相似文献
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D. Bailey D. Tirrell O. Vogl 《Journal of polymer science. Part A, Polymer chemistry》1976,14(11):2725-2747
Four new derivatives of 5-vinylsalicylic acid were prepared and their homopolymerization and copolymerization with acrylic acid and methacrylic acid investigated. Methyl 5-vinylsalicylate was prepared in a six-step synthesis from methyl salicylate in an overall yield of 35%. Acetylation in the last step yielded methyl 5-vinylacetylsalicylate. Hydrolysis of methyl 5-vinylsalicylate gave 5-vinylsalicylic acid which was acetylated to 5-vinylacetylsalicylic acid (5-vinyl aspirin). The 5-vinyl-substituted salicylic acid derivatives could be readily homopolymerized and copolymerized with acrylic acid and methacrylic acid to give various compositions of copolymers. It is worth noting that even the monomers with free phenol groups could be readily polymerized with azobisisobutyronitrile as radical initiator to high molecular weight polymers without interference of the phenolic OH group. 相似文献
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Ishibashi K Nakajima K Sugioka Y Sugiyama M Hamada T Horikoshi H Nishi T 《Chemical & pharmaceutical bulletin》1999,47(2):226-240
A series of 2-phenylbenzofuran derivatives with a carbamoyl, alkylamino, or alkyloxy group at the 5 or 6 position of the benzofuran ring were synthesized and evaluated for rat and human testosterone 5 alpha-reductase inhibitory activities in vitro. Against rat enzyme, the carbamoyl derivatives had more potent inhibitory activities than the alkylamino or alkyloxy derivatives, and the 6-carbamoyl derivatives tended to be more potent than the 5-carbamoyl derivatives. Against human enzyme, the 6-substituted derivatives had more potent inhibitory activities than the 5-substituted derivatives. The 6-carbamoyl and 6-alkylamino derivatives tended to show stronger inhibitory activities against human type 1 enzyme than against type 2 enzyme, but they were not largely selective. 相似文献
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V. P. Shchipanov I. Ya. Postovskii E. I. Rysakova 《Chemistry of Heterocyclic Compounds》1968,4(2):161-163
In order to study the connection between the structure of sulfanilamides and their antibacterial action, sulfanilamide derivatives of 1- and 2-methyl-5-aminotetrazoles and of 1,3-dimethyl-5-iminotetrazole have been synthesized. A study of their IR spectra has shown that 1-methyl-5-sulfanilimidotetrazole has the imide structure in the crystalline state and 2-methyl-5-sulfanilamidotetrazole the amide structure. The sulfanilamide derivatives of 1- and 2-methyl-5-aminotetrazoles possess a considerable antibacterial activity, while 1, 3-dimethyl-5-sulfanilimidotetrazole is inactive. 相似文献
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The reaction of trifluoropyruvic acid hydrate with urea derivatives affords 5-hydroxy-5-trifluoromethylhydantoin derivatives in good yield. The product orientation is consistent with the initial attack on the most active center, in trifluoropyruvic acid hydrate, towards nucleophiles 相似文献
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The biological versatility of aristeromycin (carbocyclic adenosine) is limited by accompanying cytotoxicity caused ostensibly by the intracellular formation of its 5'-nucleotide derivatives. Aristeromycin derivatives that offered steric interference to this transformation at the C-5' center were sought. This paper describes the facile stereospecific synthesis, where necessary, of such C-5'-methylated aristeromycin derivatives. 相似文献
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γ-Radiolysis of 5-fluorouracil and 5-fluorouridine derivatives having sulfur-containing substituents
Tokuyuki Kuroda Koji Hisamura Hiroshi Nishikawa Nobuhiro Nakamizo Yoshio Otsuji 《Journal of heterocyclic chemistry》1994,31(2):335-339
γ-Radiolysis reactions of eight 5-fluorouracil (5-FU) derivatives having sulfonyl group-containing substituents at the 1-position and five 5-fluorouridine (5-FUR) derivatives having thioureido group-containing substituents were studied under the conditions where hydrated electron (eaq?) and hydroxyl radical (HO·) become the principal reactive species. The 5-FU and 5-FUR derivatives were radiolyzed to give 5-FU and 5-FUR, respectively. The efficiency of the reactions depended upon the nature of reactive species and also upon the nature of substituents. The reactivity features of the γ-radiolysis reactions are discussed. 相似文献