共查询到20条相似文献,搜索用时 31 毫秒
1.
2.
5-(1-芳基-1-吡咯-2-基)-1氢-四唑类化合物的合成与表征 总被引:1,自引:0,他引:1
利用阳极氧化反应, 将一系列N-芳基吡咯电氰化, 区域专一地得到吡咯氰化物2, 分离收率为76%~85%. 将其与叠氮化钠反应, 合成了一系列具有潜在血管紧张素Ⅱ受体(AT)拮抗活性的新型四唑化合物. 该合成路线的原料易得, 并以阳极氰化芳香氮杂环引入氰基为关键步骤, 可作为在芳香氮杂环上引入四唑基团的通用合成路线. 相似文献
3.
Nesterova O. M. Zarubina O. S. Tolstyakov V. V. Danagulyan G. G. Trifonov R. E. Smirnov S. N. Slepukhin P. A. Ignatenko N. K. Ostrovskii V. A. 《Russian Journal of Organic Chemistry》2017,53(11):1766-1768
Russian Journal of Organic Chemistry - New tetrazolyl derivatives of pyrimidine were synthesized containing various linker groups. The structure of these compounds was established by NMR... 相似文献
4.
5.
6.
超声辐射下合成1-[(未)取代苯酰基-3-[5-(1-苯基-3-甲基-5-氯吡唑-4-基)-1,3,4-噻二唑-2-基]-硫脲 总被引:2,自引:0,他引:2
1-苯基-3-甲基-5-氯吡唑-4-甲酸与氨基硫脲在三氯氧磷中反应得到2-氨基-5-(1-苯基-3-甲基-5-氯吡唑-4-基)-1,3,4-噻二唑(1), 然后分别采用超声辐射法和常规加热法与(未)取代苯甲酰基异硫氰酸酯(2)反应合成了一系列未见报到的1-[(未)取代苯酰基-3-[5-(1-苯基-3-甲基-5-氯吡唑-4-基)-1,3,4-噻二唑-2-基]-硫脲(3a~3j). 化合物的结构经元素分析, IR, 1H NMR确证. 相似文献
7.
8.
Xing Zhou LI Xian Ping DAI Jun Hai XIAO Song LI* Beijing Institute of Pharmacology & Toxicology Beijing School of pharmaceutical Engineering Shenyang Pharmaceutical University Shengyang 《中国化学快报》2005,16(9):1137-1139
For discovering novel small molecule inhibitors of transforming growth factor-β1(TGF-β1)type-I receptor(ALK5),we designed1,3,5-triaryl-4-hydroxyl-4,5-dihydro-1H-pyrazole(1)as target compound,mimic the structure of SB-431542which is a2-pyridyl substituted triarylimiazole inhibitor of ALK51.Racemic compound1showed moderate ALK5inhibitory activity in luciferase reporter assays[inhibition(%control):0.1umol/L8.79%;1umol/L19.05%].To investigate the influence of the absolute configuration of… 相似文献
9.
10.
The title compound(zifaxaban 2, C20H16ClN3O4 S, Mr = 429.87) was synthesized and its crystal structure was determined by single-crystal X-ray diffraction. Zifaxaban crystallizes in monoclinic, space group P21 with a = 5.7900(12), b = 13.086(3), c = 12.889(3) A, β = 100.86(3)°, V = 959.1(3) A3, Z = 2, Dc = 1.489 g/cm3, F(000) = 444, μ = 0.342 mm-1, the final R = 0.0320 and wR = 0.0640 for 2717 observed reflections(I 2σ(I)). The absolute configuration of the stereogenic center in the title compound was confirmed to be S by single-crystal X-ray diffraction. Four existing intermolecular hydrogen bonds help to stabilize the lattice and the molecule in the lattice to adopt an L-shape conformation. Zifaxaban was slightly more active than rivaroxaban 1 in in vitro assay against human FXa and therefore is promising as a drug candidate. 相似文献
11.
Koteswara Rao Ch. P. Rao T. B. Charan G. Kali Srinu B. Maturi S. R. 《Russian Journal of General Chemistry》2019,89(5):1023-1028
Russian Journal of General Chemistry - In the present study a new series of 2-{4-[5-(5-substituted arylpyrimidin-2-yl)-1H-pyrazol-3-yl] phenyl}thiazolo[4,5-b]pyridine derivatives (11a–11j)... 相似文献
12.
V. V. Tkachev Yu. A. Sayapin I. V. Dorogan V. S. Gorkovets A. A. Kolodina V. N. Komissarov G. V. Shilov S. M. Aldoshin V. I. Minkin 《Russian Journal of Organic Chemistry》2013,49(3):439-445
Acid-catalyzed reaction of 6,10a-dihydroxy-3,4a,7,9-tetra(tert-butyl)-1,2,4a,10a-tetrahydrodibenzo-[b,e][1,4]dioxine-1,2-dione with 4-chloro-2,7,8-trimethylquinoline gave previously unknown 3,6,8-tri-tert-butyl-3-[2-tert-butyl-5-(4-chloro-7,8-dimethylquinolin-2-yl)-4-hydroxy-3-oxopenta-1,4-dien-1-yl]-5-hydroxy-1,4-benzodioxin-2-one whose structure was determined by X-ray analysis. The energy and structure parameters of possible isomers of the product in the gas phase and in solution were estimated by PBE0/6-31G** quantum-chemical calculations. 相似文献
13.
14.
DongMeiCAI MinJieLI DaLiangLI TianPaYOU 《中国化学快报》2004,15(2):163-166
Novel C-nucleosides of tiazofurin analogue (2-[2-(hydroxymethyl)-1,3-dioxolan-5-yl] 1,3-thiazole-4-carboxamide) and its thiol-substituted derivative (2-[2-(mercaptomethyl)-1,3-dioxolan-5-yl] 1, 3-thiazole-4-carboxamide) were synthesized from methyl acrylate through a multistep procedure. Their structures were confirmed by IR, ^1HNMR, ^13CNMR and elemental analysis. 相似文献
15.
In the course of studies on hybrid antibacterials incorporating 2-aryl-5-nitro-1H-indole moieties as potential bacterial NorA efflux pump inhibitors, the compound 1-[2-(5-nitro-1H-indol-2-yl)phenyl]methylpyridinium chloride (2) was synthesized and structurally characterized. This pyridinium chloride salt crystallized in the monoclinic space group P2(1)/c with the following unit cell dimensions: a 10.274(3) ?, b 13.101(4) ?, c 13.439(4) ?, b 107.702(7)°, V 1723.2(9) ?3, Z (f.u.) = 4; R1 = 0.048, and wR2 = 0.13. Of interest in the single crystal X-ray structure is the (intramolecular) disposition of the pyridinium plane over the indole heterocyclic residue [interplanar dihedral angle 17.91(4)°]. 相似文献
16.
Jianguang Zhou Xingxian Gu Shuping Yao Jiong Ye Peng Fu Siqian Liu Darija Dedic Fabrice Gallou 《Helvetica chimica acta》2023,106(3):e202200186
A scalable and environmentally benign route to the free base of branaplam, a small molecule splicing modulator, was identified and developed. This alternative approach circumvented the inherent risk of dioxin formation associated with ortho-halo phenol derivatives present in the previous route. A Friedel–Crafts approach provided a reliable access to the key intermediate, subsequently followed by a Suzuki–Miyaura cross-coupling. Multiple process aspects of the synthetic approach were evaluated, and a robust process for its large-scale synthesis was developed and successfully demonstrated. 相似文献
17.
Nasakin O. E. Kazantseva M. I. Varkentin L. I. Gein V. L. 《Russian Journal of General Chemistry》2018,88(6):1270-1272
Russian Journal of General Chemistry - 1-[2-(1H-indol-3-yl)ethyl]-4-acetyl-3-hydroxy-5-phenyl-1H-pyrrole-2(5H)-ones were synthesized by the short heating of a mixture of tryptamine, aromatic... 相似文献
18.
S. A. Osadchii M. D. Stanescu V. I. Mamatyuk V. G. Shuhin 《Russian Chemical Bulletin》1996,45(2):381-383
The 1-hydroxy-2-(5H-dibenzo[a,d]cyclohepten-5-yl)-1-phenylethyl cation generated under long life conditions undergoes fragmentation to afford 5H-dibenzo[a,d]cycloheptenyl-and methylphenylhydroxycarbinyl canons but does not undergo carbocationic cyclization.Translated fromIzvestiya Akademii Nauk. Seriya Khimicheskaya, No. 2, pp. 397–399, February, 1996. 相似文献
19.
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
20.
Starting from readily available 1-methyl-5-nitroimidazole-2-carboxylic acid hydrazide (1), 1-methyl-2-(1,3,4-thiadiazol-2-yl)-5-nitroimidazole (4) and 1-methyl-2-(1,3,4-oxadiazol-2-yl)-5-nitroimidazole (10) were prepared. The reaction of 1 with formic acid gave 1-(1-methyl-5-nitroimidazole-2-carboxyl)-2-(formyl)hydrazine ( 8 ) in high yield. Refluxing of the latter with phosphorus pentasulfide in xylene yielded compound 4 in 50% yield. Reaction of compound 8 with phosphorus pentoxide afforded compound 10 in 60% yield. 相似文献