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1.
Potential chelating-forming ligands and reagents for heterocyclization — ethyl esters of 4-[N-(R-pyrid-2-yl)carbamoyl]-3-amino-2-cyanobuten-2-oic acids ["codimers" of cyanoacetic acid ethyl ester (EECA) and the corresponding (pyrid-2-yl) amides of this same acid) — were synthesized in two ways: by condensation of 2-dialkylborylamidopyridines (picolines) with EECA (via chelate compounds of boron) and by the reaction of EECA dimer with 2-aminopyridines (picolines).N. D. Zelinskii Institute of Organic Chemistry, Russian Academy of Sciences, 117913 Moscow. Translated from Izvestiya Akademii Nauk, Seriya Khimicheskaya, No. 2, pp. 371–376, February, 1992. 相似文献
2.
D. Bevk M. Kmetic S. Recnik J. Svete L. Golic A. Golobic B. Stanovnik 《Chemistry of Heterocyclic Compounds》2001,37(12):1498-1510
Ethyl (Z)-2-(2,3-dihydro-1,3-dioxo-1H-isoindol-2-yl)-3-(dimethylamino)propenoate was prepared in one step from ethyl (2,3-dihydro-1,3-dioxo-1H-isoindol-2-yl)acetate and bis(dimethylamino)-tert-butoxymethane and treated with various amines and hydrazines to afford the corresponding amino substituted products. Reactions of the titled compound with N,N'-, C,N-, and C,O'-ambident nucleophiles in refluxing acetic acid furnished the corresponding fused pyrimidinones, quinolizinones, and pyranones. 相似文献
3.
Letafat B Emami S Mohammadhosseini N Faramarzi MA Samadi N Shafiee A Foroumadi A 《Chemical & pharmaceutical bulletin》2007,55(6):894-898
As a part of continuing search for potential antibacterial agents in the quinolones field, we have synthesized novel quinolone agents bearing N-[2-(thiophen-3-yl)ethyl] piperazinyl moiety in the 7-position of the quinolone ring. In vitro antibacterial evaluation of the target compounds showed that N-[2-(thiophen-3-yl)ethyl] group attached to piperazine ring served as promising C-7 substituent for piperazinyl quinolone antibacterials. Among these derivatives, ciprofloxacin analogues, containing N-[2-(thiophen-3-yl)-2-hydroxyiminoethyl] or N-[2-(thiophen-3-yl)-2-methoxyiminoethyl] residue provided a high inhibition against all the tested Gram-positive organisms including methicillin-resistant Staphylococcus aureus comparable or superior with respect to the reference drugs norfloxacin and ciprofloxacin. 相似文献
4.
In the reaction of N-[2-(5-bromouracil-1-yl)ethyl]alkylamines with alkylamines at 40 °C kine-substitution takes place with the formation of N-[2-(6-alkylamino-uracil-1-yl)ethyl]alkylamines.Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 9, pp. 1260–1261, September, 1984. 相似文献
5.
V. A. Dorokhov S. V. Baranin A. Dib K. L. Cherkasova M. N. Bochkareva V. S. Bogdanov 《Russian Chemical Bulletin》1992,41(4):765-769
New chelating ligands, N-(pyrid-2-yl)amides of 4,4,4-trichloro-3-amino-2-cyanocrotonic acid have been synthesized from N-(pyrid-2-yl)amides of cyanoacetic acid and CCl3CN. It has been demonstrated that by the action of butylthiodibutylborane they form binuclear boron chelate complexes. Analogous chelates have also been obtained from the N-(pyrid-2-yl)amides of acetoacetic and 4,4,4-trichloro-3-aminocrotonic acids.N. D. Zelinskii Institute of Organic Chemistry, Russian Academy of Sciences, Moscow 117913. Translated from Izvestiya Akademii Nauk, Seriya Khimicheskaya, No. 4, pp. 974–979, April, 1992. 相似文献
6.
Although nitrogen-containing heterocycles and sulfonamides both play crucial roles in the chemical and pharmaceutical industries, surprisingly little research exists that examines the bifunctional N-(2-(pyridin-2-yl)ethyl)sulfonamide scaffold for any potential applications. Retrosynthetic analysis indicates that this skeleton would be well suited for a conjugate addition reaction. However, the ability of 2-vinylpyridine to behave as an acceptor, and of sulfonamides to behave as donors, has very limited literature precedent, and thus required some preliminary investigations into their mutual reactivity. Herein outlines our laboratory's discovery of a novel and efficient solvent-free 1,4-aza-conjugate addition reaction between sulfonamides and 2-vinylpyridines that provides expedient access to various N-(2-(pyridin-2-yl)ethyl)sulfonamide derivatives. The products, possessing multiple sites of Brønsted acidity and basicity in close proximity, could display a wide array of valuable host–guest properties and should thus be investigated for potent pharmaceutical or agrochemical properties.
[Supplementary materials are available for this article. Go to the publisher's online edition of Synthetic Communications® for the following free supplemental resource(s): Full experimental and spectral details.] 相似文献
7.
以N-吡啶基吡唑甲酸和2-氨基-3-甲基苯甲酸为起始原料,经由亲核加成、环化和酰化等多步反应合成了一系列结构新颖的N-(2-(5-(3-溴-1-(3-氯吡啶-2-基)-1H-吡唑-5-基)-1,3,4-噁二唑-2-基)-4-氯-6-甲基苯基)酰胺类化合物.测试了所合成化合物的杀虫及抑菌活性,结果表明,新化合物大多化合物在200 mg·L^-1浓度下对东方粘虫(Mythimna separataWalker)具有一定的杀虫活性,尤其是N-(2-(5-(3-溴-1-(3-氯吡啶-2-基)-1H-吡唑-5-基)-1,3,4-噁二唑-2-基)-4-氯-6-甲基苯基)乙酰胺(8a)和N-(2-(5-(3-溴-1-(3-氯吡啶-2-基)-1H-吡唑-5-基)-1,3,4-噁二唑-2-基)-4-氯-6-甲基苯基)-3-氯-2,2-二甲基丙酰胺(8e)致死率可达70%;部分化合物在50 mg·L^-1浓度下对油菜菌核病菌的抑菌活性相对较好(54.5%~63.6%),优于triadimefon和chlorantraniliprole;部分化合物如N-(2-(5-(3-溴-1-(3-氯吡啶-2-基)-1H-吡唑-5-基)-1,3,4-噁二唑-2-基)-4-氯-6-甲基苯基)-3,3-二甲基丁酰胺80和N-(2-(5-(3-溴-1-(3-氯吡啶-2-基)-1H-吡唑-5-基)-1,3,4-噁二唑-2-基)-4-氯-6-甲基苯基)-4-氟苯甲酰胺(8h)对苹果轮纹病菌具有中等抑菌活性.值得注意的是,化合物8e的杀粘虫活性和对油菜菌核病菌的抑菌活性都较为突出,可用作新农药创制研究的新型参考结构. 相似文献
8.
L. G. Lavrenova A. R. Amamchyan S. V. Larionov V. A. Dorokhov 《Russian Chemical Bulletin》1992,41(10):1810-1812
We have synthesized complex compounds of Co(2+) chloride with hydrochlorides of N-(1,2,4-triazol-5-yl)benzamidine and N-(tetrazol-5-yl)benzamidine. According to magnetochemistry and electron spectroscopy data, the ligands are coordinated in a bidentate fashion with the N atom of the amidine group and the N atom of the heterocycle with formation of the tetrahedral chromophore CoN2Cl2.Institute of Inorganic Chemistry, Siberian Branch, Russian Academy of Sciences, 630090 Novosibirsk. N. D. Zelinskii Institute of Organic Chemistry, Russian Academy of Sciences, 117913 Moscow. Translated from Izvestiya Akademii Nauk, Seriya Khimicheskaya, No. 10, pp. 2311–2315, October, 1992. 相似文献
9.
V. S. Bogdanov S. V. Baranin A. Dib I. P. Yakovlev V. A. Dorokhov 《Russian Chemical Bulletin》1991,40(1):147-151
Chelate complexes in which the boron atom is bound to the pyridine N atom and the O atom of the deprotonated ligand were synthesized by reaction of N-(pyrid-2-yl)- and N-(4-methylpyrid-2-yl) cyanoacetamides. A new type of intrachelate tautomeric transformation was discovered: the complexes obtained can exist in solutions in the form of two tautomers, which are derivatives of acetimidic acid or the corresponding ketene N,O-acetals.Translated from Izvestiya Akademii Nauk SSSR, Seriya Khimicheskaya, No. 1, pp. 164–168, January, 1991. 相似文献
10.
T Suzuki H Inagaki H Hamajima H Uesaka K Hori T Ikami 《Chemical & pharmaceutical bulletin》1999,47(6):880-883
Three metabolites of N-[2-(1-azabicyclo[3.3.0]octan-5-yl)ethyl]-2-nitroaniline fumarate (SK-946), a novel central muscarinic cholinergic receptor agonist, were prepared to confirm their proposed structures, and tested for muscarinic receptor affinity in vitro. 相似文献
11.
Ravinaik B. Rao M. V. B. Rao P. T. S. R. K. P. Ramachandran D. Reddy D. R. S. 《Russian Journal of Organic Chemistry》2021,57(4):624-630
Russian Journal of Organic Chemistry - A series of substituted N-(4-{5-[4-(5-methyl-1,3,4-oxadiazol-2-yl)phenyl]-4-(2,3,4-trimethoxyphenyl)-1,3-thiazol-2-yl}phenyl)benzamides were designed... 相似文献
12.
V. A. Shadrikova E. V. Golovin E. A. Kuznetsova M. Yu. Rostova Yu. N. Klimochkin 《Russian Journal of Organic Chemistry》2016,52(10):1452-1462
Quaternary 1-[2-(adamantan-1-yl)ethyl]pyridinium bromides were reduced with sodium tetrahydridoborate in ethanol, and hydroarylation of the resulting 1-[2-(adamantan-1-yl)ethyl]-1,2,3,6-tetrahydropyridines with benzene in trifluoromethanesulfonic acid afforded phenylpiperidines with preferentially equatorial orientation of the phenyl substituent. 相似文献
13.
Baichurin R. I. Reshetnikov A. A. Sergeev V. D. Aboskalova N. I. Makarenko S. V. 《Russian Journal of General Chemistry》2019,89(5):865-869
The condensation of 3-(furan-2-yl)- and 3-(thiophen-2-yl)prop-2-enals with nitro-substituted CH acids, namely ethyl nitroacetate, nitroacetone, nitroacetophenone, and nitroacetonitrile, afforded a series of geminally activated nitro dienes, 4-(furan-2-yl)- and 4-(thiophen-2-yl)-1-nitrobuta-1,3-dienes. The product structure was confirmed by NMR and IR spectroscopy.
相似文献14.
Guido Sello Silvana Bernasconi Fulvia Orsini Patrizia Di Gennaro 《Tetrahedron: Asymmetry》2009,20(5):563-565
The cascade use of enzymatic activities allows for the preparation of enantiomerically pure epoxides. In particular, using whole-cell biocatalysts we can prepare both (?)-[3-(oxiran-2-yl)phenyl]methanol and (?)-3-(oxiran-2-yl)benzoic acid in one-pot, two or three steps procedure. The yield is quantitative and enantiomeric purity greater than 95%. The selected biocatalysts contain a styrene monoxygenase from Pseudomonas fluorescens ST and a naphthalene dihydrodiol dehydrogenase from P. fluorescens N3, cloned and expressed in Escherichia coli. 相似文献
15.
Methods of selective methylation of the nitrogen atoms of the ethyl ester of 3-(1H-imidazol-4-yl)-2-propenoic acid are reported. The nitrogen atom α to the ethylenic chain was methylated after protection of the β nitrogen with a phenacyl group. 相似文献
16.
Yu. O. Remizov L. M. Pevzner M. L. Petrov A. I. Ponyaev 《Russian Journal of General Chemistry》2015,85(12):2728-2734
By cyclization of carboethoxyhydrazone of ethyl 4-acetyl-5-methylfuran-2-carboxylate under the conditions of Hurd–Mori reaction ethyl 4-(1,2,3-thiadiazol-4-yl)-5-methylfuran-2-carboxylate was synthesized. The ester obtained was brominated with N-bromosuccinimide at the methyl group in the furan ring. This bromide reacts with various N-, S-, O-, and P-nucleophiles to form the corresponding substitution products. Furylthiadiazole fragment remains stable in the course of these transformations. 相似文献
17.
I. O. Tupaeva Yu. A. Sayapin Zyong Ngia Bang V. N. Komissarov V. V. Tkachev G. V. Shilov S. M. Aldoshin V. I. Minkin 《Russian Chemical Bulletin》2013,62(2):492-496
An acid-catalyzed reaction of 2-methylbenzoxazole with 3,4,5,6-tetrachloro-1,2-benzoquinone leads to 2-(benzoxazol-2-yl)-5,6,7-trichloro-1,3-tropolone and 2-(benzoxazol-2-yl)-4,5,6,7-tetrachloro-1,3-tropolone. 1,3-Tropolones upon reflux in ethyl alcohol undergo the rearrangement resulted in the seven-membered ring contraction to form ethyl 2-(benzoxazol-2-yl)-5,6-dichloro-3-hydroxybenzoate and ethyl 2-(benzoxazol-2-yl)-4,5,6-trichloro-3-hydroxybenzoate. The molecular structure of the latter was established by X-ray diffraction analysis. 相似文献
18.
Prakash TP Manoharan M Kawasaki AM Lesnik EA Owens SR Vasquez G 《Organic letters》2000,2(25):3995-3998
[structure] Oligonucleotides with two novel modifications, 2'-O-?2-[N, N-(dimethyl)aminooxy]ethyl? (2'-O-DMAOE) and 2'-O-?2-[N, N-(diethyl)aminooxy]ethyl? (2'-O-DEAOE), have been synthesized. These modifications exhibit high binding affinity to target RNA (and not to DNA) and enhance the nuclease stability of oligonucleotides considerably with t(1/2) > 24 h as a phosphodiester. 相似文献
19.
20.
Transformations of the derivatives of 2-substituted 5-(1,2,3-thiadiazol-4-yl)-3-furoic acid under the action of bases has been studied. In the presence of potassium tert-butylate in THF, the studied compounds decompose with the cleavage of the thiadiazole ring, liberation of nitrogen, and formation of labile acetylene thiolates. In the presence of methyl iodide, these salts form stable 2-methylthioethynylfurans. Under the action of sodium ethylate in ethanol, thiadiazole ring of ethyl [2-methyl-5-(1,2,3-thiadiazol-4-yl)]-3-furoate is split to form the corresponding sodium acetylene thiolate. Under the action of ethanol, two molecules of this salt give bis(furyl)dithiafulvene. In the DMF–potassium carbonate system, acetylene thiolates react with primary and secondary amines giving thioamides of (4-ethoxycarbonyl-5-methylfur-2-yl)acetic acid. Treating of ethyl 2-methyland 2-N-morpholinomethyl-5-(1,2,3-thiadiazol-4-yl)-3-furoates with hydrazine hydrate leads to hydrazinolysis of the ester group and cleavage of thiadiazole ring resulting in the formation of hydrazides of 4-hydrazinocarbonylfur-2-ylacetic acid. In the case of ethyl 2-acetoxymethyl- and 2-(4-nitrophenoxy)methyl-5-(1,2,3-thiadiazol-4-yl)-3-furoates, thiadiazole ring is retained and exclusively hydrazinolysis of the ester groups is observed. 相似文献