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1.
Slowinski F Ben Ayad O Vache J Saady M Leclerc O Lochead A 《The Journal of organic chemistry》2011,76(20):8336-8346
Azabicyclo[2.2.1]heptane and -[3.3.1]nonane scaffolds (X = Cl, Br) containing a pyridinyl substituent at the bridgehead position were prepared via two complementary chemical pathways, either by the transformation of a methoxy group into a synthetically valuable chlorine atom at the C-6 position of the pyridine moiety or by means of a regioselective C-6 deprotonation/halogenation process of the pyridine moiety exemplified by chlorination or bromination. These newly generated scaffolds were then engaged in Suzuki-Miyaura coupling reactions to provide α7 nicotinic ligands. Both chemical series were evaluated in vitro for their affinity at α7 nicotinic receptors, revealing nanomolar potency with significant selectivity over the α4β2 nicotinic subtype. These approaches offer a general access to these α7 nicotinic scaffolds and ligands. 相似文献
2.
Amr A. E. Abdalla M. M. Essaouy S. A. Areef M. M. H. Elgamal M. H. Nassear T. A. Haschich A. E. 《Russian Journal of General Chemistry》2017,87(8):1826-1833
Russian Journal of General Chemistry - A number of substituted 4-methoxy-7-methyl-6-(substituted methyl)-5-oxo-5H-furo[3,2-g]-chromene-9-sulfonates 3a–3f and 4a–4c were synthesized.... 相似文献
3.
5-, 2-Methylbicyclo[2.2.1]hept-2-enes, 2-methylenebicyclo[2.2.1]heptane were synthesizedby a new procedure, and their transformations in a flow system over stationary layer of aluminosilicatecatalyst were studied at various temperatures. At 150-400°C these compounds undergo isomerization which is accompanied by -migration of hydrogen. The isomerization mechanism is discussed in terms of formation of classical carbocations, not invoking nonclassical carbenium ion. 相似文献
4.
Synthesis and in vitro evaluation of new diphenyl ether derivatives as serotonin transporter ligands
《中国科学B辑(英文版)》2008,(5)
For the development of new ligands as potential imaging agents for the serotonin transporter (SERT),a series of diphenyl ether derivatives have been synthesized,characterized,and evaluated for their in vitro binding affinities to the SERT. Among the above compounds,2-(2-((dimethylamino)methyl)-4-fluoro-phenoxy)-5-bromobenzenamine (15) and 2-(2-((dimethylamino)methyl)-4-fluorophenoxy)-5-iodobenzene amine (16) show high binding affinities for the SERT with Ki values of 0.28 and 0.20 nmol·L-1,respectively. They can be further labeled with carbon-11,fluorine-18,iodine-123 or bromine-76,and evaluated as useful imaging agents for the SERT. Moreover,the study of the structure-activity relationship (SAR) provides some useful information for the future design of new ligands. 相似文献
5.
The interaction of 2,6-disubstituted bicyclo[3.3.1]nonanes with - and -cyclodextrins has been investigated by1H NMR spectroscopy and the formation of (11) host—guest complexes has been established.Translated fromIzvestiya Akademii Nauk. Seriya Khimicheskaya, No. 12, pp. 2523–2525, December, 1995. 相似文献
6.
M. M. Krayushkin V. V. Sevost’yanova V. N. Yarovenko I. V. Zavarzin 《Russian Chemical Bulletin》2009,58(10):2175-2177
Reaction of bicyclo[3.3.1]nona-3,7-diene-2,6-dione with nitroform in boiling methanol occurs with involvement of the solvent
and results in 2,6-dimethoxy-4,8-bis(trinitromethyl)-bicyclo[3.3.1]nona-2,6-diene, while the reaction in tert-butyl alcohol affords 4,8-bis(trinitromethyl)bicyclo[3.3.1]nona-2,6-dione. 相似文献
7.
Hosoya M Otani Y Kawahata M Yamaguchi K Ohwada T 《Journal of the American Chemical Society》2010,132(42):14780-14789
Helical structures of oligomers of non-natural β-amino acids are significantly stabilized by intramolecular hydrogen bonding between main-chain amide moieties in many cases, but the structures are generally susceptible to the environment; that is, helices may unfold in protic solvents such as water. For the generation of non-hydrogen-bonded ordered structures of amides (tertiary amides in most cases), control of cis-trans isomerization is crucial, even though there is only a small sterical difference with respect to cis and trans orientations. We have established methods for synthesis of conformationally constrained β-proline mimics, that is, bridgehead-substituted 7-azabicyclo[2.2.1]heptane-2-endo-carboxylic acids. Our crystallographic, 1D- and 2D-NMR, and CD spectroscopic studies in solution revealed that a bridgehead methoxymethyl substituent completely biased the cis-trans equilibrium to the cis-amide structure along the main chain, and helical structures based on the cis-amide linkage were generated independently of the number of residues, from the minimalist dimer through the tetramer, hexamer, and up to the octamer, and irrespective of the solvent (e.g., water, alcohol, halogenated solvents, and cyclohexane). Generality of the control of the amide equilibrium by bridgehead substitution was also examined. 相似文献
8.
Ya. A. Gur’eva I. N. Alekseev O. A. Zalevskaya P. A. Slepukhin A. V. Kutchin 《Russian Journal of Organic Chemistry》2016,52(6):781-784
New enantiomerically pure Schiff bases and palladium chelates based thereon were synthesized starting from (–)-α-pinene or (?)-camphor and N,N-dimethylethane-1,2-diamine. 相似文献
9.
Yan-Chun Guo Jing Li Jiao-Li Ma Zhi-Ran Yu Hai-Wei Wang Wen-Juan Zhu Xin-Cheng Liao Yu-Fen Zhao 《中国化学快报》2015,26(6):755-758
Two series of thieno[2,3-d]pyrimidine derivatives were designed and synthesized, in which bioactive a-aminophosphonate subunits were introduced at the N3 position through an N–N bond connection.The in vitro cytotoxic activity of the novel compounds was tested against human esophageal carcinoma cells(EC109), human hepatocarcinoma cells(Hep G2), human gastric carcinoma cells(MGC-803),respectively, by the MTT method. The evaluation results revealed that compounds 6mb, 6mf, 6mg, 6nd and 6nh exerted the most potent inhibition against Hep G2, MGC-803 and EC109 cells, respectively. In particular, compound 6mg presented excellent inhibitory effect against Hep G2(91.2%) and MGC-803(94.4%) cells. 相似文献
10.
11.
A. B. Zolotoi P. M. Lukin S. V. Konovalikhin M. Yu. Skvortsova O. E. Nasakin L. O. Atovmyan 《Chemistry of Heterocyclic Compounds》1991,27(4):413-419
The problems of the structure—property interrelationship of 3-imino-2-oxabicyclo[2.2.1]heptane derivatives are discussed on the basis of x-ray diffraction studies (XDS). A pathway for the formation of the bicyclic compounds is proposed, and the realization of spirans in the reaction of sym-tetracyanoethane with conjugated cyclic systems containing s-cis C=C and C=O fragments is substantiated. The factors responsible for the syn orientation of the oxygen atom and the N-substituent of the imino group are analyzed. It is shown that a change in the steric hindrance in the bicyclic compounds leads to a change in the conformation of the latter. The reasons for the shortening of the Csp3-Csp3, Csp3-Csp and C=N exo bonds and the correlation of the XDS and IR spectroscopic data are examined. From the XDS data for N-bromo-substituted imines, a model for Br+...NC electrophilic attack was proposedCommunication 16 from the series Chemistry of 1,1,2,2-tetracyanoethane. See [1] for Communication 15.Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 4, pp. 519–526, April, 1991. 相似文献
12.
S. A. Pogosyan Dzh. A. Avakimyan H. M. Stepanyan 《Russian Journal of Organic Chemistry》2016,52(9):1308-1311
Methods have been developed for the synthesis of new heterocyclic systems, spiro[chromene-4,3′- indoles] and spiro[indole-3,4′-quinolines] by the base-catalyzed domino reaction of isatins with 5,5-dimethylcyclohexane- 1,3-dione (or 5,5-dimethyl-3-anilinocyclohex-2-en-1-one) and ethyl cyanoacetate. 相似文献
13.
In our synthetic studies toward huperzine A, a diastereoselective α′-alkylation of the α-amido-γ-methyl hexenone 4 was realized through a dianion intermediate which significantly enhanced the reactivity. Under the attempted Heck reaction conditions, an unexpected and unprecedented palladium-catalyzed intramolecular γ-arylation of 3 was observed, which generated 18 with bicyclo[3.3.1]nonane framework in satisfactory yield. 相似文献
14.
Xue Fei Yang Ling Yi Kong 《中国化学快报》2007,18(4):380-382
A series of 2-aryl-5-alkyl-7-methoxylbenzo[b]furan derivatives have been synthesized by utilizing the coupling of methyl 3-methoxy-4-hydroxy-5-bromocinnamate with cuprous phenylacetylide as the key step.The structures of the new compounds were confirmed by1H NMR,IR and MS.The structure of compound 14 was further confirmed by single crystal X-ray.Compound 17 showed cytotoxic activity against human lung carcinoma A549. 相似文献
15.
Kumar KS Kumar PM Kumar KA Sreenivasulu M Jafar AA Rambabu D Krishna GR Reddy CM Kapavarapu R Shivakumar K Priya KK Parsa KV Pal M 《Chemical communications (Cambridge, England)》2011,47(17):5010-5012
Concurrent construction of five and six membered fused N-heretocyclic ring was achieved via a conceptually new three-component reaction affording 6,6a-dihydroisoindolo[2,1-a]quinazoline-5,11-diones as novel inhibitors of TNF-αin vitro. This represents one of the few examples of direct TNF-α inhibition by small molecules. 相似文献
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17.
《中国化学快报》2017,(2)
New series of pyrazolo[1,5-α]pyrimidine derivatives 7a-i,11a-c and Schiff bases 13a-c were synthesized and screened for their in vitro antitumor activity against three human carcinoma cell lines,namely colorectal carcinoma(HCT116),prostate adenocarcinoma(PC-3) and liver carcinoma(HepG-2) using MTT cytotoxicity assay at 100 μg/mL.Some of the tested compounds displayed good anticancer activities against HCT-116 and PC-3 cells.Whereas,compounds 7d and 11 a showed better antitumor activity than the rest of the compounds against both cell lines.A structure-activity relationship(SAR) has been discussed and structures of the newly synthesized compounds were confirmed by different spectral data(MS,IR,~1H NMR and ~(13)C NMR) and elemental analysis. 相似文献
18.
19.
The C-alkylation of cyclic α-nitroketones with α-halobenzyl halides in the presence of DBU followed by a Pd-catalyzed intramolecular C-arylation afforded benzo-and naphtho-fused bicyclo[n.3.1]alkane derivatives (n = 3, 4, 5) in excellent overall yields for the two-step sequence. In some of the reactions starting from α-nitrocyclooctanone, the major products were fused indane derivatives arising from an intramolecular attack of an intermediate Pd species onto the carbonyl group, followed by elimination. 相似文献
20.
Sofiane Ben Sdira Marie-Béatrice Giudicelli Francis Vocanson Monique Perrin Roger Lamartine 《Tetrahedron letters》2005,46(34):5659-5663
A new family of p-tert-butylcalix[4]arenes functionalized at the lower rim with α-ketoamide or α-hydroxyamide functions has been prepared. The 1H and 13C NMR spectra indicate that the macrocycles preferably adopt a cone conformation. X-ray crystal study of the α-ketoamide derivative 4a shows the flattened cone conformation in the solid state. Reduction of α-ketoamide 4ab has produced the α-hydroxyamide derivatives 6ab. The introduction of chiral moieties on the lower rim position of the calix[4]arene allowed the synthesis of the chiral derivatives 7 and 8. Host-guest complexation properties towards various anions of the chiral α-hydroxyamide 8 have been examined by 1H NMR spectroscopy. This new receptor has shown promising selectivity for and N-tosyl-(L)-alaninate. 相似文献