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The reaction of 2-carboethoxyethyl-4,5-dimethoxybenzene sulfochloride with substituted pyridines leads to the corresponding sulfonamides. The latter were hydrolysed to the acids, on which a general method for preparing a new ring system was based. 相似文献
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Rg Bader 《Helvetica chimica acta》1968,51(6):1409-1420
1, 2-Dithioles with sulfur substitutents in position 5 are prepared by reaction of 4-chloro-1, 2-dithiol-3-ones with thiols, sulfinates, dithiocarbamates, or potassium ethylxanthate. Bis-(4-chloro-1, 2-dithiol-3-on-5-yl) sulfide is produced from 4, 5-dichloro-1, 2-dithiol-3-one with sodium thiosulfate and other thiol forming reagents. The 5-alkylthio- and 5-arylthio-1, 2-dithiol-3-ones can be oxidized with peracids to sulfoxides and, partly, to sulfones; the sulfones can also be obtained from sulfinates. 4-Chloro-5-(α-methyl-benzylthio)-1, 2-dithiol-3-one reacts differently with peracetic acid, giving bis-(4-chloro-1, 2-dithiol-3-on-5-yl) disulfide besides 4-chloro-1, 2-dithiol-3-one. With oxalyl chloride, 4-chloro-5-alkylthio-1, 2-dithiol-3-ones form 3, 4-dichloro-dithioliumchlorides, which react with anilines to give 3-phenylimino-4-chloro-5-alkylthio-1, 2-dithioles. 相似文献
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5-亚环己基-2-取代氨基咪唑啉酮类化合物的合成及其杀菌活性研究 总被引:1,自引:0,他引:1
以环己酮和2-硫代乙内酰脲为起始原料,经Knoevenagel缩合反应制得5-亚环己基-2-硫代咪唑啉-4-酮(1),化合物1在乙醇钠/乙醇体系中与碘甲烷反应得到5-亚环己基-2-甲硫基咪唑啉-4-酮(2),化合物2再与相应的取代苯胺或苄胺在冰醋酸体系中回流制得目标化合物5-亚环己基-2-取代氨基咪唑啉酮3a~3r,它们的化学结构经1H NMR,IR,MS和X-ray单晶衍射确证.5-亚环己基-2-对氯苄氨基咪唑啉酮(3q):Mr=335.83,C16H18ClN3O CH4O,Monoclinic,P2(1)/n,ρ=1.264 g/cm3,F(000)=712,Z=4,a=0.59895(12)nm,b=1.2161(2)nm,c=2.4289(5)nm,β=94.03(3)°.初步生物活性测定结果表明:在50μg/mL浓度下,部分目标化合物均对供试菌种显现出一定的抑制活性,其中5-亚环己基-2-对氟苄氨基咪唑啉酮(3p)对油菜菌核的EC50为24.37μg/mL,3q对辣椒疫霉的EC50为28.68μg/mL. 相似文献
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为寻找活性强、作用时间长的新型非肽类血管紧张素II AT1受体拮抗剂, 从易得原料3-烷基-4,5-二氢-1-(3-氯-4-氟苯基)-1,2,4-三唑-5-酮出发, 经过N-烃化反应、1,3-偶极反应、氢解、水解和酰化等反应, 合成得到一系列4-取代-3-烷基-4,5-二氢-1-(3-氯-4-氟苯基)-1,2,4-三唑-5-酮类衍生物, 总收率为58%~87%, 其结构经IR, 1H NMR, MS和元素分析确证. 初步药理试验结果表明: 所有目标化合物均有一定的AT1受体拮抗活性, 其中化合物12d抑制AII诱导的兔主动脉环收缩的IC50值为4.0×10-9 mol/L, 与阳性药坎地沙坦(candesartan)相当, 具有进一步的研究意义. 相似文献
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新型2-氨基-5-苯亚甲基-4H-咪唑啉-4-酮衍生物的合成及生物活性 总被引:12,自引:0,他引:12
通过烯基膦亚胺1与芳基异氰酸酯的aza-Wittig反应得到碳二亚胺2,再用2与亲核试剂的成环反应制得10个新型的2-氨基-5-苯亚甲基-4H-咪唑啉-4-酮衍生物4,探讨了碳二亚胺2与不同亲核试剂反应的活性并分离得到了一个胍中问体3i,初步研究了化合物4的生物活性. 相似文献
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High selectivity has been discovered for the C-alkylation of ambident anions of 5-oxo-1H-4,5-dihydroindeno[1,2-b]pyridines with ethyl bromoacetate, allyl, propargyl, and phenacyl bromides, which leads to the formation of the corresponding 4a-substituted 5-oxo-4H-4a,5-dihydroindeno[1,2-b]pyridines in high yield. 相似文献
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Guang Xin XIA Jian Feng LI Shun An LAI Ai Ming PENG Shu Jun ZHANG Xiao Hui WEI Xin Jian CHEN Jing Shan SHEN Ru Yun JI 《中国化学快报》2005,16(10):1283-1286
A novel series of pyrido[ 1,2-e]purin-4(3H)-one derivatives containing polar substituents on 5'-position were designed and prepared as potential PDE5 inhibitors. This paper reports the synthetic routes, 1H-NMR data, and the PDE5 inhibitory activities of the target compounds. The polar piperazinyl group contained (on 5'-position) compound, 3B2, showed the highest activity among the tested derivatives but less potency than sildenafil 1. 相似文献
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UV-Irradiation of 4-bromo-3-methyl-l-phenyl-4,5-dihydro-pyrazol-5-one (1) in the presence of various aromatic hydrocarbons gave different types of photoproducts depending on the nature of the hydrocarbons via an electron-transfer mechanism. In the presence of naphthalene or phenanthrene a photochemical homocoupling reaction of 1 occurred to form 2 or 2 and 3, respectively. 相似文献
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Kataeva O. N. Litvinov I. A. Krivolapov D. B. Lodochnikova O. A. Abdel-Hafez Sh. H. Movchan A. I. Chmutova G. A. 《Russian Journal of General Chemistry》2003,73(5):776-781
The structure of acylamino derivatives of 1-(2,4,6-trichlorophenyl)-4,5-dihydropyrazol-5-one was studied by X-ray diffraction. 3-Acetylamino-1-(2,4,6-trichlorophenyl)-4,5-dihydropyrazol-5-one and 3-benzoylamino-1-(2,4,6-trichlorophenyl)-4,5-dihydropyrazol-5-one exist in crystal as CH tautomers. The nature and number of acylamino groups were found to affect the nature of intermolecular hydrogen bonds in the crystals studied. 相似文献
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9-Hydroxypyrido[1,2-a]pyrimidin-4-one ( 5 ) was prepared by condensation of 2-amino-3-hydroxypyridine with isopropylidene aminomethylenemalonate. The reaction first led to an enaminoester intermediate which underwent cyclization by heating at 250° affording the new heterocyclic phenol 5 . A similar condensation performed on 2-amino-3-benzyloxypyridine yielded the corresponding benzylic ether which can be easily debenzylated to 5 by hydrogenolysis. Furthermore 2-amino-3-benzyloxypyridine condensed with diethyl ethoxymethylenemalonate gave 9-benzyloxy-3-ethoxycarbonylpyrido[1,2-a]pyrimidin-4-one which was also debenzylated to the corresponding free phenol. 相似文献
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Movchan A. I. Kurbangalieva A. R. Kataeva O. N. Litvinov I. A. Chmutova G. A. 《Russian Journal of General Chemistry》2003,73(7):1130-1136
A single-crystal X-ray diffraction study showed that 1-phenyl-3-methyl-4-formyl-4,5-dihydropyrazol-5-one occurs in the solid phase as two conformers of the NH tautomer. The acidity and basicity constants of 1-phenyl-3-methyl-4-formyl-4,5-dihydropyrazol-5-one and its analog, -5-thione, in 50% aqueous dioxane were measured. PM3 calculations qualitatively explan the differences in the tautomerism and acid-base properties of 4-formylpyrazolone (-pyrazolethione) and the corresponding compounds without the formyl substituent. 相似文献
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A gold(I)-catalyzed regioselective method for the preparation of 3-bromo/iodo-tetrahydropyran-4-one derivatives from homopropargyl acetal is reported. A one-pot procedure based on a gold(I)-catalyzed Petasis–Ferrier rearrangement/cyclization and subsequent electrophilic halogenation was developed. Corresponding hemiacetals were not suitable substrates for the formation of the 3-halo-pyran derivatives. The present transformation is a useful method to readily afford highly substituted 3-halo-tetrahydropyran-4-ones, which are suitable substrates in a variety of reactions in further synthesis. 相似文献
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The reaction of 1,2-diamino-4,5-diphenylimidazole with 1,3-diarylpropenones and 1,3-diaryl-2,3-dibromopropenones gives dihydro- and heteroaromatic derivatives of 6-hydroxyimidazopyrimidines and also imidazopyrimidines which do not contain the 6-hydroxy group. It was found that the structure of the products depended on the conditions for carrying it the reaction. 相似文献
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Bao Xiang Hu Zhen Lu Shen Jun Lu Xin Quan Hu Wei Min Mo Nan Sun 《Phosphorus, sulfur, and silicon and the related elements》2013,188(2):523-535
The synthesis of some new functionalized thiazolidin-4-one derivatives has been described. The N-substituted-thiosemicarbazides 3a-3i were obtained though the reaction of alkylamines 2a–2i , carbon disulfide, and hydrazine hydrate. The condensation reaction between 3a–3i and 4-amino-2-methanesulfanylpyrimidine-5-carboxaldehyde 1 afforded the thiosemicarbazones 4a–4i . The corresponding thiazolidin-4-ones 5a–5i were prepared by cyclization of 4a–4i with ethyl bromoacetate. The structures of the final products were confirmed by IR, 1 H NMR, 13 C NMR, and HRMS. 相似文献