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1.
Krivopalov V. P. Bushuev M. B. Gatilov Yu. V. Shkurko O. P. 《Russian Chemical Bulletin》2010,59(9):1808-1816
The reactions of pyrimidine-2-carbonitrile and 4,6-dimethylpyrimidine-2-carbonitrile with hydrazine hydrate were investigated.
Intermediates in the route of successive transformations of pyrimidine-2-carbonitrile (pyrimidine-2-carbamidrazone and 1,2-bis[amino(pyrimidin-2-yl)methylidene]hydrazine)
into trinuclear heterocyclic compounds, viz., symmetrical di(pyrimidin-2-yl)-1,4-dihydro-1,2,4,5-tetrazines and di(pyrimidin-2-yl)-4H-1,2,4-triazol-4-amines (potential polydentate ligands), were isolated. The oxidative dehydrogenation of di(pyrimidin-2-yl)-1,4-dihydro-1,2,4,5-tetrazines
afforded the corresponding 3,6-di(pyrimidin-2-yl)-1,2,4,5-tetrazines. 相似文献
2.
Avetisyan A. A. Aleksanyan I. L. Ambartsumyan L. P. 《Russian Journal of Organic Chemistry》2010,46(4):568-570
1-(2-Methylquinolin-4-yl)thiocemicarbazides and S-(2-methylquinolin-4-yl)thiosemicarbazide hydrochlorides were synthesized by reaction of 6(8)-substituted 4-chloro-2-methylquinolines
with thiosemicarbazide under different conditions. Alkaline hydrolysis of the hydrochlorides afforded substituted 1-(2-methylquinolin-4-yl)thiosemicarbazides. 相似文献
3.
E. V. Koroleva K. N. Gusak Zh. V. Ignatovich A. L. Ermolinskaya M. P. Bei A. P. Yuvchenko 《Russian Journal of Organic Chemistry》2012,48(8):1121-1125
Acylation of 6-methyl-N-[4-(pyridin-3-yl)pyrimidin-2-yl]benzene-1,3-diamine, 4-methyl-N-[4-(pyridin-3-yl)pyrimidin-2-yl]benzene-1,3-diamine, and N-[4-(pyridin-3-yl)pyrimidin-2-yl]benzene-1,3-diamine with maleopimaric and citraconopimaric acid chlorides, with benzotriazolyl maleopimarate afforded N-[3-(pyrimidin-2-yl)aryl]amides of maleopimaric and citraconopimaric acids. By the reaction of substituted N-arylamides of maleopimaric acid with methanesulfonic acid biologically active methanesulfonates were obtained. 相似文献
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A. A. Aghekyan G. G. Mkryan A. S. Tsatinyan O. S. Noravyan G. V. Gasparyan 《Russian Journal of Organic Chemistry》2017,53(3):362-365
Treatment of 1-(4-chlorobenzylamino)-2-methylpropan-2-ol with concentrated sulfuric acid at 0°C gave 6-chloro-4,4-dimethyl-1,2,3,4-tetrahydroisoquinoline which reacted with (aryloxymethyl)oxiranes to afford new propan-2-ol derivatives of the tetrahydroisoquinoline series, 1-(aryloxy)-3-(6-chloro-4,4-dimethyl-1,2,3,4-tetrahydroisoquinolin-2-yl)propan-2-ols. Some of the synthesized compounds or their hydrochlorides showed moderate adrenergic blocking and sympatholytic activities. 相似文献
7.
R. I. Vas'kevich Yu. L. Zborovskii V. I. Staninets A. N. Chernega 《Russian Journal of Organic Chemistry》2004,40(7):1047-1052
4-Aryl-1-(4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl)thiosemicarbazides react with dimethyl acetylenedicarboxylate in methanol to give the corresponding methyl {3-aryl-4-oxo-2-[(4-oxo-3,4-dihydro-thieno[2,3-d]pyrimidin-2-yl)hydrazono]-1,3-thiazolidin-5-ylidene}acetates, whereas in dioxane methyl 5-aryl-amino-2-methoxycarbonylmethyl-3-(4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl)-2,3-dihydro-1,3,4-thiadiazole-2-carboxylates are mainly formed. 相似文献
8.
A. Yu. Potapov Kh. S. Shikhaliev M. A. Potapov M. A. Prezent D. Yu. Vandyshev 《Russian Journal of Organic Chemistry》2017,53(7):1060-1065
Cyclization of 3-(dimethylamino)-1-(2,2,4,6-tetramethyl-1,2,3,4-tetrahydroquinolin-7-yl)prop-2-en-1-one with carboximidamides, guanidines, and 1,2,4-triazol-5-amines afforded a number of new 2,2,4,6-tetramethyl-7-(2-R-pyrimidin-4-yl)-1,2,3,4-tetrahydroquinolines and 2,2,4,6-tetramethyl-7-(2-R-[1,2,4]triazolo-[1,5-a]pyrimidin-7-yl)-1,2,3,4-tetrahydroquinolines. 相似文献
9.
A. V. Ivashchenko O. N. Garicheva L. V. Shmelev Yu. S. Ryabokobylko G. M. Adamova 《Chemistry of Heterocyclic Compounds》1980,16(12):1275-1278
The previously unknown 3-[4(3H)-pyrimidinon-2-yl]amino-1H-1,2,4-triazoles, which were converted to 3-[4-chloro-, 3-(4-ethoxy)-, 3-(4-hydrazinopyrimidin-2-yl)]-amino-2(4)H-1,2,4-triazoles, were obtained by the reaction of 2-nitroamino-4(3H)-pyrimidinones with 3-amino-5-hexyl-1H-1,2,4-triazole. The condensation of the initial products with -diketones gave 3-[4-(1H-pyrazol-1-yl)pyrimidin-2-yl]-amino-2(4)H-1,2,4-triazoles. The IR, UV, and PMR spectra of the synthesized compounds were studied.Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 12, pp. 1678–1681, December, 1980. 相似文献
10.
D. E. Stepanov L. V. Grishchuk R. Yu. Ivanova Yu. E. Ivanov A. A. Yavolovskii G. L. Kamalov 《Russian Journal of General Chemistry》2013,83(3):526-529
The synthesis of 2-(2-amino-4-arylthiazol-5-yl)pyrimidin-4(3H)-ones from the available 2-(2-oxo-2-arylethylidene)-2,3-dihydropyrimidin-4(1H)-ones was developed. 相似文献
11.
N′-(取代嘧啶-2-基)-N-菊酰硫脲的合成与生物活性研究 总被引:7,自引:0,他引:7
采用活性基团拼接法, 将第一菊酸构型中的最高活性组分(+)-反式菊酸以及二氯菊酸引入到含取代嘧啶环的酰基硫脲结构中, 合成了5个未见文献报道的N′-(取代嘧啶-2-基)-N-(+)-反式菊酰硫脲衍生物(3a~3e)和3个均未见文献报道的N′-(取代嘧啶-2-基)-N-二氯菊酰硫脲(3f~3h), 结构经元素分析、IR和1H NMR得到确证. 初步的生物活性测试结果表明: 大部分化合物具有较好的杀菌活性, 有的化合物兼具除草和杀菌活性, 有的化合物兼具杀虫和杀菌活性. 相似文献
12.
Synthesis of Novel 2-(Pyridin-2-yl) Pyrimidine Derivatives and Study of Their Anti-Fibrosis Activity
Yi-Fei Gu Yue Zhang Feng-li Yue Shao-tong Li Zhuo-qi Zhang Jing Li Xu Bai 《Molecules (Basel, Switzerland)》2020,25(22)
A pyrimidine moiety exhibiting a wide range of pharmacological activities has been employed in the design of privileged structures in medicinal chemistry. To prepare libraries of novel heterocyclic compounds with potential biological activities, a series of novel 2-(pyridin-2-yl) pyrimidine derivatives were designed, synthesized and their biological activities were evaluated against immortalized rat hepatic stellate cells (HSC-T6). Fourteen compounds were found to present better anti-fibrotic activities than Pirfenidone and Bipy55′DC. Among them, compounds ethyl 6-(5-(p-tolylcarbamoyl)pyrimidin-2-yl)nicotinate (12m) and ethyl 6-(5-((3,4-difluorophenyl)carbamoyl)pyrimidin-2-yl)nicotinate (12q) show the best activities with IC50 values of 45.69 μM and 45.81 μM, respectively. Furthermore, the study of anti-fibrosis activity was evaluated by Picro-Sirius red staining, hydroxyproline assay and ELISA detection of Collagen type I alpha 1 (COL1A1) protein expression. Our study showed that compounds 12m and 12q effectively inhibited the expression of collagen, and the content of hydroxyproline in cell culture medium in vitro, indicating that compounds 12m and 12q might be developed the novel anti-fibrotic drugs. 相似文献
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A. V. Yudina A. G. Mazhuga E. K. Beloglazkina I. V. Yudin I. A. Rodin N. V. Zyk 《Russian Chemical Bulletin》2011,60(10):2120-2123
A reaction of potassium ({(4Z)-4-[(1-methyl-1H-imidazol-2-yl)methylene]-5-oxo-1-phenyl-4,5-dihydro-1H-imidazol-2-yl}thio)acetate with copper(II) chloride in methanol leads to bis(5-anilino-7-methoxycarbonyl-1-methyl-1H-imidazo[1,2-c]pyrimidin-4-ium) tetrachloro-cuprate(II), whose structure was confirmed by the X-ray diffraction studies. 相似文献
15.
A. T. Baryshnikova B. F. Minaev G. V. Baryshnikov W. -H. Sun 《Russian Journal of Inorganic Chemistry》2016,61(5):588-593
On the basis of X-ray crystallographic data on molecular copper complexes with 1,3-bis(3-(pyrimidin-2-yl)-1H-1,2,4-triazol-5-yl)propane, quantum-chemical optimization of their equilibrium structure has been performed by the density functional theory method with subsequent analysis of the electron density distribution by Bader’s atoms in molecules method and g-factor anisotropy calculation. The topological parameters of electron density at the Cu–N bond critical points have been considered, and the bond energies have been estimated using the Espinosa equation. A phenomenon of variable coordination of nitrate ions with Cu(II) ions in the inner coordination sphere of the mononuclear copper complex with 1,3-bis(3-(pyrimidin-2-yl)-1H-1,2,4-triazol-5-yl)propane has been revealed. The contributions of different components to the gfactor anisotropy have been analyzed in the framework of the gauge-independent atomic orbital method. The largest contribution to the g-factor is made by the orbital (Zeeman) and spin–orbit components accounting for very high averaged g-factor values of 2.1413 and 2.5636 for the doublet state of the mononuclear complex and the triplet state of the binuclear complex, respectively. 相似文献
16.
N-[4-(3-Methoxyphenyl)pyrimidin-2-yl]cyanamide ( 1 ) was reacted with morpholine and respective binuclephilic reagents namely: ethylenediamine, o-phenylenediamine, o-aminothiophenol, or o-aminophenol to give the corresponding carboximidamide 2 , imidazolidine 3 , and benzazoles 4–6 . While its reaction with hydrazides in DMF at 90°C, gave the corresponding 1,2,4-triazols 7–11 . Also, treatment of cyanamide 1 with heterocycles having both nucleophilic and electrophilic groups (─NH2/─COOEt) in iso-propanol in presence of catalytic amount of Conc. HCl, gave the corresponding thieno[2,3-d]pyrimidinone 12 and unexpected thieno[3,2-d]pyrimidine 13 instead of bis-thieno[3,2-d]pyrimidine 14 , respectively. While, its reaction with ethyl 5-amino-1,3-thiazole-4-carboxylate yielded the unexpected N-(pyrimidin-2-yl)urea 15 rather than the corresponding thiazolo[5,4-d]pyrimidine 16 . Unexpected N-(pyrimidin-2-yl)thiourea 17 was obtained, when cyanamide 1 reacted with potassium thiolates in iso-propanol with catalytic amount of Conc. HCl. 相似文献
17.
Yoshifumi Watanabe Hirotaka Yoshiwara Munefumi Kanao 《Journal of heterocyclic chemistry》1993,30(2):445-451
The syntheses of 4-(benzo[b]furan-3-yl)piperidines, 4-(benzo[b]furan-2-yl)piperidines and 4-(benzo[b]thiophen-3-yl)piperidines with 5-HT2 antagonist activity are described. Reaction of 1-acetyl-4-(2,4-difluorobenzo-yl)piperidine 2 with methyl glycolate gave methyl 6-fluoro-3-(1-acetylpiperidin-4-yl)benzo[b]furan-2-carboxylate 3 , which was converted to 2-[2-[4-(benzo[b]furan-3-yi)piperidin-1-yl]ethyl-5,6,7,8-tetrahydro-1,2,4-triazolo-[4,3-a]pyridin-3(2H)-one hydrochloride 9 . Analogous benzo[b]furans 17a-d and benzo[b]thiophenes 10a,b and 18a were prepared by a similar method. Cyclization of 4-fluoro-2-(4-pyridinylmethoxy)acetophenones 20a,b afforded 4-(benzo[b]furan-2-yl)pyridines 21a,b , which were converted to 2-[2-[4-(benzo[b]furan-2-yl)-piperidin-1-yl]ethyl-5,6,7,8-tetrahydro-1,2,4-triazolo[4,3-a]pyridin-3(2H)-one hydrochlorides 24a,b. Among them, benzo[b]furans 9 and 17a,d and benzo[b]thiophenes 10 and 18a showed potent 5-HT2 antagonist activity in vitro. 相似文献
18.
4-Arylaminomethylene-3-methyl-1-(6-methyl-4-oxo-1,4-dihydropyrimidin-2-yl)pyrazol-5(4H)-ones were synthesized by a three-component reaction between the 6-methyl-2-(3-methyl-5-oxo-2,5-dihydropyrazol-1-yl)pyrimidin-4(1H)-one, triethoxymethane, and an aromatic amine. These compounds were found to exist as aminomethyleneketones regardless of
the electronic effects of substituents in the aromatic fragments. The resulting compounds showed pronounced tuberculocidic
activity. 相似文献
19.
Samuel D. Banister Shane M. WilkinsonRaphy Hanani Aaron J. ReynoldsDavid E. Hibbs Michael Kassiou 《Tetrahedron letters》2012,53(29):3780-3783
A practical, multigram approach to the 2-(2-(4-alkoxyphenyl)-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)acetamide (DPA) class of ligands targeting the translocator protein (TSPO) is described. This synthetic route offers several improvements over all previously described sequences, including the isolation of intermediates without resort to chromatography. The common precursor to the DPA class of high affinity TSPO ligands, N,N-diethyl-2-(2-(4-hydroxyphenyl)-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)acetamide, was produced in 40% yield over six steps, and was cleanly alkylated to give multigram quantities of several DPA analogues in 90-96% yield after recrystallization. 相似文献
20.
N. S. Prostakov A. A. Obynochnyi L. A. Murugova 《Chemistry of Heterocyclic Compounds》1987,23(5):544-547
Condensation of 3-methyl-2-azafluorene with 2-formylfluorene results in the formation of a compound containing a polyconjugated system and two acidic CH centers, namely, 1-(fluoren-2-yl)-2-(2-azafluoren-3-yl)ethene. The conversions of this compound upon treatment with alkali have been studied by electronic absorption spectroscopy. The methyl iodide derivative of this base was used as an intermediate in the preparation of a pseudo-azulene, 1-(fluoren-2-yl)-2-(2H, 2-methylindeno[2,3-c]pyridine)ethene.Translated from Khimiya Geterotsiklicheskikh Soedinenii No. 5, pp. 657–659, May, 1987. 相似文献