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1.
Ethyl 3-halo-2-propynoates undergo facile (no heating, no base, no solvent) palladium- and copper-free cross-coupling with 4,5,6,7-tetrahydroindoles on alumina to afford the corresponding 4,5,6,7-tetrahydroindole-2-propynoates in 46% and 71% yields. The yield of the by-products [ethyl 3,3-di(4,5,6,7-tetrahydro-1H-indol-2-yl)acrylates] under appropriate conditions can reach 79%. 相似文献
2.
Boris A. Trofimov Lyubov N. Sobenina Zinaida V. Stepanova Olga V. Petrova Igor A. Ushakov Albina I. Mikhaleva 《Tetrahedron letters》2008,49(24):3946-3949
4,5,6,7-Tetrahydroindoles undergo a rapid, facile (rt, 60 min) ethynylation with ethyl 3-halo-2-propynoates upon grinding with solid K2CO3 (without solvent) at C-2 of the tetrahydroindole ring to afford ethyl 3-(4,5,6,7-tetrahydroindol-2-yl)-2-propynoates in 62–90% yield. 相似文献
3.
Lyubov' N. Sobenina Vladislav N. Drichkov Al'bina I. Mikhaleva Olga V. Petrova Igor A. Ushakov Boris A. Trofimov 《Tetrahedron》2005,61(20):4841-4849
5-Amino-3-(pyrrol-2-yl)isoxazoles were selectively prepared by the reaction of 2-(2,2-dicyano-1-ethylthioethenyl)pyrroles with hydroxylamine in methanol. Under analogous conditions, 2-(2-carbamoyl-2-cyano-1-ethylthioethenyl) pyrroles with hydroxylamine gave 5-aminoisoxazoles and their structural isomers, 3-aminoisoxazoles (3-5% yield). The latter were selectively prepared by reacting 2-(2-carbamoyl-2-cyano-1-ethylthioethenyl)pyrroles with hydroxylamine in the presence of aqueous NaOH and from the products of intramolecular cyclization of 2-(2-carbamoyl-2-cyano-1-ethylthioethenyl)pyrroles, 1-ethylthio-3-iminopyrrolizines and hydroxylamine. 相似文献
4.
Di(4,5,6,7-tetrafluorobenzothiazol-2-yl) disulfide, obtained by oxidation of 2-mercapto-4,5,6,7-tetrafluorobenzothiazole,
readily reacts with aliphatic and alicyclic amines to form the corresponding sulfenyl amides.
Dedicated to the memory of Academician N. N. Vorozhtsov on the 100th anniversary of his birth.
Published in Russian in Izvestiya Akademii Nauk. Seriya Khimicheskaya, No. 6, pp. 1225–1226, June, 2007. 相似文献
5.
A new method for the synthesis of N-substituted 2-(4-oxo-4,5,6,7-tetrahydroindol-3-yl)acetic acids was developed. Alkylation of cyclic 1,3-diketones with 3,5,5,5-tetrachloropentan-2-one affords 1,4-diketones, which undergo cyclization with different primary amines into N-substituted 3-(2,2,2-trichloroethyl)-4,5,6,7-tetrahydroindol-4-ones. Acid hydrolysis of the latter gives the corresponding indol-3-ylacetic acids. The structures of the compounds obtained were confirmed by 1H and 13C NMR data. 相似文献
6.
V. T. Abaev M. G. Kadieva A. V. Butin G. D Krapivin E.T. Oganesyan V. E. Zavodnik 《Chemistry of Heterocyclic Compounds》2000,36(11):1261-1271
Methods were developed for the synthesis of 3-butyl-2-(3-oxobutenyl)benzofurans and 3-(3-furylbenzofuran-2-yl)acrylic acids on the basis of 3-furyl-2-(3-oxobutyl)benzofurans. 相似文献
7.
Xin Bo ZHOU Cui Fang LIN Song LI 《中国化学快报》2005,16(10):1301-1304
The synthesis of (S)-2-(3-arylacrylamido)-3-{4-[2-(5-methyl-2-phenyloxazol-4-yl)etho- xy]phenyl}propanoic acids is described. Their structures were confirmed by ^1H-NMR. 相似文献
8.
AbstractHerein, we describe a one-pot synthesis of some novel 2-(3-alkyl/aryl-5-trifluoromethylpyrazol-1-yl)-4-(coumarin-3-yl)thiazoles (6) involving the reaction of 3-alkyl/aryl-5-hydroxy-5-trifluoromethyl-4,5-dihydropyrazole-1-thiocarboxamides (3) with 3-bromoacetylcoumarins (5) in the presence of sodium carbonate in ethanol. Reaction of 3 with 5 in the absence of sodium carbonate, however, resulted in the formation of 2-(3-alkyl/aryl-5-hydroxy-5-trifluoromethyl-4,5-dihydropyrazol-1-yl)-4-(coumarin-3-yl)thiazoles, which were subsequently dehydrated to 6 by refluxing in ethanol in the presence of sodium carbonate. The structure of the synthesized compounds (6) was confirmed by infrared (IR), mass, 1H NMR, and 13C NMR spectra and elemental analysis data. Newly synthesized compounds (6) showed moderate to good activity against Gram-positive bacteria. 相似文献
9.
The 13C NMR spectra of twelve 3-aryl-4-(5-aryl-Δ2-l,2,4-oxadiazolin-3-yl)sydnones and twelve 3-aryl-4-(5-aryl-l,2,4-oxadiazol-3-yl)sydnones have been measured and assigned by means of proton-noise decoupling and DEPT-experiments. The coupling constants were determined by means of gated decoupling, and NOE effects were observed by comparison of proton-decoupled and inverse-gated decoupled spectra. Differences shown by the oxadiazoline and the oxadiazole rings and the substitution effects are discussed. 相似文献
10.
L. A. Kayukova K. M. Beketov A. L. Akhelova K. D. Praliev 《Chemistry of Heterocyclic Compounds》2006,42(7):914-917
Cyclization of O-benzoyl-2-(benzimidazol-1-yl)propioamidoxime under different temperature conditions gave 2-[2-(5-phenyl-1,2,4-oxadiazol-3-yl)ethyl]benzimidazole
whose structure has been determined by X-ray analysis.
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Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 7, pp. 1057–1061, July, 2006. 相似文献
11.
1-[5-(1,3-二氧-4,5,6,7-四氢-1H-异吲哚-2-基)苯基]-3-取代脲衍生物的合成与除草活性研究 总被引:1,自引:0,他引:1
为了寻找高效低毒的原卟啉原氧化酶抑制剂(protox)类除草剂, 设计并合成了一系列1-[5-(1,3-二氧-4,5,6,7-四氢-1H-异吲哚-2-基)苯基]-3-取代脲类衍生物4a~4d和5a~5g. 化合物4a~4d经异氰酸酯法合成, 收率、纯度高; 化合物5a~5g利用固体光气一锅法合成, 反应时间短.所得化合物结构经1H NMR, IR, 质谱和元素分析表征. 初步生物活性测试表明: 化合物4c, 5a, 5b, 5c在有效成分75 g/hm2 剂量下对苘麻、马刺苋、凹头苋等双子叶杂草表现出90%以上的防效. 相似文献
12.
设计合成了系列光系统II (PS-II)电子传递抑制剂2-氰基-3-(2-氟吡啶-5-基)甲氨基-3-甲硫基氰基丙烯酸酯类化合物. 其结构经1H NMR、元素分析确证. 生物活性测定表明: 部分化合物显示出很好的除草活性. 其中活性最好的化合物在150 g/ha, 对阔叶杂草的防效在90%以上. 构效关系研究表明: 氰基丙烯酸酯的3位取代基对它们的活性影响较大. 3位由(2-氟吡啶-5-基)甲氨基取代的氰基丙烯酸酯和相应的氯取代的氰基丙烯酸酯的除草活性相当或稍高. 相似文献
13.
(E)-N-芳基-3-[2-(8-羟基喹啉基)-乙烯基]咔唑的合成、抗氧化活性及促进鼠骨髓间质干细胞增殖的研究 总被引:4,自引:0,他引:4
设计合成了3-[2-(8-羟基喹啉基)-乙烯基]-N-对甲苯基咔唑(8)和3-[2-(8-羟基喹啉基)-乙烯基]-N-对甲氧苯基咔唑(9)两个新的化合物, 用IR, MS, 1H NMR和元素分析确认其结构. 并利用DPPH8226;方法, 超氧阴离子自由基( )法, 羟基自由基HO8226;法和噻唑蓝比色法(MTT法)分别测定了目标产物的抗氧化活性和调控鼠骨髓间质干细胞(MSCs)的作用. 结果表明, 这两种化合物对DPPH8226;自由基、超氧阴离子自由基和羟基自由基具有较强的抗氧化活性, 化合物9在低浓度时对鼠骨髓间质干细胞增殖有很好的促进作用. 相似文献
14.
O. V. Shablykina O. V. Khilya V. V. Ishchenko V. P. Khilya 《Chemistry of Natural Compounds》2005,41(5):529-532
3-(2-Quinolyl)- and 3-(5-carbethoxyfuryl-2)coumarins were prepared by reaction of substituted salicylaldehydes and hetarylacetonitriles.
Alkylation and acylation of 3-hetaryl-7-hydroxycoumarins were studied.
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Translated from Khimiya Prirodnykh Soedinenii, No. 5, pp. 432–434, September–October, 2005. 相似文献
15.
Yu. M. Volovenko A. V. Tverdokhlebov T. A. Volovnenko 《Chemistry of Heterocyclic Compounds》2001,37(7):876-884
The reaction of 2-(2-azahetaryl)-3-oxo-4-chlorobutyronitriles with substituted benzaldehyde hydrazones gives 4-arylideneamino-2-(1-R-benzimidazol-2-yl)-3-oxobutyronitriles, the structures of which were proved using spectroscopic data, the results of elemental analysis, and through their chemical reactions. It was found that the reaction course depends on the basicity of the heterocyclic fragment in the starting nitrile. A likely mechanism for the process is proposed. 相似文献
16.
The title compound ethyl 2-(6-(1,3-dioxo-4,5,6,7-tetrahydro-1H-isoindol-2(3H)-yl)-7-fluoro-3-oxo-2H-benzo[b][1,4]oxazin-4(3H)-yl) butanoate 3 was synthesized by the reaction of ethyl 2-(6-amino-7-fluoro-3-oxo-2H-benzo[b][1,4]oxazin-4(3H)-yl) butanoate with 4,5,6,7-tetraydrophthalic anhydride,and its structure was determined by X-ray single-crystal diffraction.The crystal belongs to the monoclinic system,space group P21/n with a = 9.3469(2),b = 16.7715(5),c = 13.7153(4) ,β = 104.9680(10)°,μ = 0.107 mm-1,Mr = 430.42,V = 2077.08(10) 3,Z = 4,Dc = 1.376 g/cm3,F(000) = 904,T = 296(2) K,R = 0.0508 and wR = 0.1478. 相似文献
17.
Lyubov' N. Sobenina Ol'ga V. PetrovaDenis N. Tomilin Maxim D. GotskoIgor' A. Ushakov Lyudmila V. KlybaAl'bina I. Mikhaleva Boris A. Trofimov 《Tetrahedron》2014
2-(Furan-2-yl)- and 2-(thiophen-2-yl)pyrroles are readily ethynylated with acylbromoacetylenes in the solid Al2O3 medium (no solvent, room temperature, 1 h) to afford 5-(furan-2-yl)- and 5-(thiophen-2-yl)-2-acylethynylpyrroles in 39–74% yields. In the case of 2-(furan-2-yl)pyrroles, an alternative ethynylation of the furan ring takes place, the ratio of the furan and pyrrole ring ethynylation products being 1:5–7. No ethynylation of the thiophene ring as well as ethynylation of both heterocycles in a one molecule has been detected. Thus the reactivity of the heterocycles towards the ethynylation system (acylbromoacetylenes/Al2O3) falls in the order: pyrrole>furan>thiophene. 相似文献
18.
(Chromon-3-yl)bis(indol-3-yl)methanes and E-2-hydroxy-3-(1-methylpyrrol-2-ylmethylene)chroman-4-ones have been obtained in good yields from 3-formylchromones on reaction with indoles and N-methylpyrrole under solvent-free conditions. Reactions of (chromon-3-yl)bis(indol-3-yl)methanes with guanidine carbonate and hydrazine hydrate proceed with the participation of the chromone ring system and lead to the formation of the corresponding pyrimidines and pyrazoles bearing the bis(indol-3-yl)methyl moiety. 相似文献
19.
20.
Nalajam Guravaiah 《合成通讯》2013,43(8):1167-1174
Reaction of phenyl acetylene with 3-(1-aryl-2-mercapto-4-imidazolyl)-2H-1-benzopyran-2-ones (4) in the presence of sodium hydroxide in absolute ethanol led to the formation of 3-(1-phenyl-2-(Z-styrylthio)-1H-imidazol-4-yl)-2H-chromen-2-ones (6) in excellent yields. These, on further oxidation with H2O2/AcOH, gave the corresponding sulfones (7) with retention of stereochemistry.