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1.
Kensuke Okuda Shigeki Takarada Takashi Hirota Kenji Sasaki 《Journal of heterocyclic chemistry》2015,52(3):780-792
Libraries of tricyclic 2‐substituted 4‐alkylamino‐9‐chloro‐5,6‐dihydropyrimido[5,4‐d]benzazepines and tetracyclic 12‐substituted 8‐chloro‐1,2,5,6‐tetrahydro‐4H‐imidazo[1′,2′:1,6]pyrimido[5,4‐d]benzazepines were synthesized as part of our research to develop new effective antiplatelet drugs. Several alkyl and aryl groups were used as substituents at the 2‐position. Evaluation of the effects of the newly synthesized compounds on collagen‐induced platelet aggregation revealed several promising antiplatelet candidates with potencies superior to aspirin. 相似文献
2.
Ag Loaded on SiO2 as an Efficient and Recyclable Heterogeneous Catalyst for the Synthesis of Chloro‐8‐substituted‐9H‐purines
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Suresh Maddila Jignesh Valand Harinarayana Bandaru Kotaiah Yalagala Palakondu Lavanya 《Journal of heterocyclic chemistry》2016,53(1):319-324
Ag support on silica has been used as an effective heterogeneous catalyst for the facile synthesis of chloro‐8‐substituted‐9H‐purine derivatives via the one‐pot reaction of 6‐chloro‐pyrimidines and substituted acids. The title compounds were formed as excellent yields with short reaction time under eco‐friendly conditions. The prepared catalyst (Ag/SiO2) can be reused for a number of times with insignificant loss in its activity. This route has the advantage of being a cost‐effective, readily available, easy workup procedure. 相似文献
3.
A. Laporterie J. Dubac G. Manuel G. Deleris J. Kowalski J. Dunogues R. Calas 《Tetrahedron》1978,34(17):2669-2673
The determining role of silicon and germanium for ene syntheses was confirmed in the reactions between 1-sila and 1-germacyclopent-3 enes or allenylsilanes and PhSO2NSO, a highly reactive new enophile. In the case of the cyclic enes the reaction led to new α,β-unsaturated β-functional cyclic derivatives which can be easily reduced into the corresponding thiols. With allenylsilanes, the adducts resulting from the ene-reaction with PhSO2NSO or 4-phenyl 1,2,4-triazoline 3,5-dione have an acetylene structure whereas the substituted allenes usually give conjugated diene derivatives. 相似文献
4.
The structure of p‐substituted phenyl 2‐nitrovinyl sulfones was studied through different spectral methods. It has been found that the nucleophilic substitution reactions of sodium phenylsulfinates with 1‐chloro‐2‐nitroethene occur stereospecifically. The formation of E‐isomers of this type of substituted phenyl vinyl sulfones was confirmed by FTIR and NMR spectroscopy. It was suggested that the E‐isomers formation was determined by the more stable conformation of the carbanionic intermediate as a result of intramolecular rotation around single Cα‐Cβ bond. This appears to be the product‐determining pathway during the interaction of sodium phenyl sulfinates with the highly activated substrate 1‐chloro‐2‐nitroethene. 相似文献
5.
《Journal of heterocyclic chemistry》2018,55(2):475-480
A new series of 4‐hetroaryl substituted quinazolines were designed and synthesized by the reaction of pentafluoro(chloro)pyridine and 2‐substituted quinazolinone. The aromatic nucleophilic substitution of pentafluoro(chloro)pyridine with quinazolinone occurs at the 4‐position of pyridine ring by the oxygen site (O‐centered nucleophile) of quinazolinone. The structures of all the compounds were confirmed by IR, 1H NMR, 19F NMR, and 13C NMR spectroscopy as well as elemental analysis. 相似文献
6.
δ‐Cyanoketones are quickly cyclized with KOtBu to 3‐aminocyclohex‐2‐enone derivatives, which in turn will give substituted indoles when treated with oxalyl chloride. Thus, 3‐amino‐6,6‐dimethylcyclohex‐2‐enone gave 3‐chloro‐6,6‐dimethyl‐2,5,6,7‐tetrahydroindole‐2,5‐dione, whose structure was corroborated by X‐ray crystallography, whereas the corresponding molecule without the blocking gem‐dimethyl groups, 3‐aminocyclohex‐2‐enone, gave via hydrogen shifts 6‐chloro‐3‐hydroxyoxindole. 相似文献
7.
Mohamed A. Khalil 《中国化学会会志》2002,49(6):1069-1072
The synthesis of different substituted pyrazolo[3,4‐b]pyridines by the reaction of 3‐amino‐5‐chloro‐1‐phenylpyrazole‐4‐carboxaldehyde 1 as starting material with some active methylene reagents has been reported. 相似文献
8.
9.
Andreas Schmidt 《Journal of heterocyclic chemistry》2002,39(5):949-956
Depending on electronically or kinetically stabilizing effects determined by the substitution pattern or the reaction conditions, 6‐amino substituted (5‐chloropyrimidine‐2,4‐diyl)bis(hetarenium) salts or 5‐chloro‐2,6‐bis‐(pyridinio)‐pyrimidin‐4‐aminides are formed on nucleophilic substitution of 4‐(dimethylamino)pyridine, 4‐(pyrrolidin‐1‐yl)pyridine, or 1‐methylimidazole on 4‐amino substituted 2,5,6‐trichloropyrimidines. 相似文献
10.
Jae‐Chul Jung Seikwan Oh Won‐Ki Kim Woo‐Kyu Park Jae Yang Kong Oee‐Sook Park 《Journal of heterocyclic chemistry》2003,40(4):617-623
A variety of 4‐substituted quinolin‐2(1H)‐ones were prepared and evaluated for N‐methyl‐D‐aspar‐tate (NMDA) receptor binding site activity and their abilities to inhibit neurotoxicity. The 4‐(2‐car‐bethoxyethanamino)‐7‐chloro‐3‐nitroquinolin‐2(1H)‐one ( 9b ) exhibited favorable NMDA receptor binding site activity and 7‐chloro‐4‐(benzylamino)‐3‐nitroquinolin‐2(1H)‐one ( 9c ) showed the most potent neurotoxicity among them. The synthetic strategies involve the use of well known keto ester condensation and reductive ring cyclization of intermediates ( 2a‐d ) to afford 4‐substituted quinolin‐2(1H)‐ones. 相似文献
11.
Synthesis and Transformations of 5‐Chloro‐2,2′‐Dipyrrins and Their Boron Complexes, 8‐Chloro‐BODIPYs
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Haijun Wang Prof. M. Graça H. Vicente Dr. Frank R. Fronczek Prof. Kevin M. Smith 《Chemistry (Weinheim an der Bergstrasse, Germany)》2014,20(17):5064-5074
Symmetric dipyrrylketones 1 a , b were synthesized in two steps from the corresponding α‐free pyrroles, by reaction with thiophosgene followed by oxidative hydrolysis under basic conditions. The dipyrrylketones produced the corresponding 5‐chloro‐dipyrrinium salts or 5‐ethoxy‐dipyrrins on reaction with phosgene or Meerwein’s salt, respectively. Boron complexation of the dipyrrins afforded the corresponding 8‐functionalized BODIPYs (borondipyrromethenes) in high yields. The 5‐chloro‐dipyrrinium salts reacted with methoxide or ethoxide ions to produce monopyrrole esters, presumably via a 5,5‐dialkoxy‐dipyrromethane intermediate. In contrast, 8‐chloro‐BODIPYs underwent a variety of nucleophilic substitutions of the chloro group in the presence of alkoxide ions, Grignard reagents, and thiols. In the presence of excess alkoxide or Grignard reagent, at room temperature or above, substitution at the boron center also occurred. The 8‐chloro‐BODIPY was a particularly useful reagent for the preparation of 8‐aryl‐, 8‐alkyl‐, and 8‐vinyl‐substituted BODIPYs in very high yields, using Pd0‐catalyzed Stille cross‐coupling reactions. The X‐ray structures of eleven BODIPYs and two pyrroles are presented, and the spectroscopic properties of the synthesized BODIPYs are discussed. 相似文献
12.
A novel and efficient strategy for the synthesis of 2‐substituted 4‐azaindoles from 2‐chloro‐3‐nitropyridine through Pd‐catalyzed Sonogashira cross‐coupling, followed by reduction and heteroannulation on t‐BuOK, is reported. 相似文献
13.
Eduardo Corts Corts Raúl Salazar Franco Olivia García Mellado 《Journal of heterocyclic chemistry》2001,38(3):663-669
A series of twelve new 2‐[(o‐ and p‐substituted)aminophenyl]‐3H‐5‐[(o‐ and p‐substituted)phenyl]‐7‐chloro‐1,4‐benzodiazepines, which have possible pharmacological properties has been obtained. The synthesis was carried out following six steps. The structure of all products was corroborated by ir, 1H nmr, 13C nmr and ms. In addition for the compound 2‐(o‐chloroaminophenyl)‐3H‐5‐(o‐fluorophenyl)‐7‐chloro‐1,4‐benzodiazepine 7, its structure was confirmed by X‐ray diffraction. 相似文献
14.
《Journal of heterocyclic chemistry》2017,54(2):1514-1521
A new method for the preparation of 2‐substituted 6‐chloro‐2,7‐dihydro‐3H‐dibenzo[de ,h ]cynnoline‐3,7‐diones has been developed. The compounds have been obtained in an original three‐step procedure comprising the oxidation of 1‐methyl‐9,10‐anthraquinones with periodate or permanganate/brominating reagent systems, cyclization to 6‐chloro‐2,7‐dihydro‐3H‐dibenzo[de ,h ]cynnoline‐3,7‐dione, and selective alkylation thereof. The selected processes were applied in the efficient scale‐up of specific 2,6‐substituted 2,7‐dihydro‐3H‐dibenz[de ,h ]cinnolin‐3,7‐dione derivatives, currently being investigated pre‐clinically as anticancer agents. 相似文献
15.
Jahangeer Patujo Amin Badshah Raja Azadar Hussain Muhammad Nawaz Tahir Shaista Tahir Muhammad Khawar Rauf 《中国化学会会志》2015,62(11):1020-1027
In the present work new nitro substituted thioureas, and their copper complexes have been synthesized and characterized by FTIR and multinuclear NMR techniques. Some of the compounds namely 1‐benzoyl‐3‐(4‐chloro‐3‐nitrophenyl) thiourea (A‐1), 1‐benzoyl‐3‐(4‐chloro‐3‐nitrophenyl) thiourea (A‐2) and 1‐benzoyl‐3‐(2‐methoxy‐4‐nitrophenyl) thiourea (A‐2) have also been characterized by single crystal XRD. All the synthesized compounds have been screened for DNA binding potencies (using cyclic voltametry, UV‐vis spectroscopy) and free radical scavanging activities. 相似文献
16.
Eduardo Corts Cortas Miryan Adaya Baos Olivia García‐Mellado De Corts 《Journal of heterocyclic chemistry》2004,41(2):277-280
A new synthesis to obtain eleven novel derivatives of 11‐[(o‐ m‐ and p‐substituted)‐phenyl]‐8‐chloro‐3,3‐dimethyl‐2,3,4,5,10,11‐hexahydro‐1H‐dibenzo[b,e][1,4]diazepin‐1‐ones with possible pharmacological activity in the central nervous system in two efficient steps has been developed. The final products were obtained by condensation and cyclization between 3‐[4‐chloro‐1,2‐phenylenediamine]‐5,5‐dimethyl‐2‐cyclohexenone with (o‐ m‐ and p‐substituted)benzaldehyde. The structure of all products was corroborated by ir, 1H‐nmr, 13C‐nmr and high resolution in ms. 相似文献
17.
A new one‐step synthesis of highly substituted thiophen‐2(3H)‐one derivatives was developed. 2‐Aryl‐1‐(morpholin‐4‐yl)ethanethiones were reacted with 2‐chloro‐2‐phenylacetyl chloride in DMF in the presence of a base to give the title compounds in moderate‐to‐good yields. 相似文献
18.
Dr. Rudy Lhermet Maha Ahmad Dr. Catherine Fressigné Dr. Bernard Silvi Dr. Muriel Durandetti Dr. Jacques Maddaluno 《Chemistry (Weinheim an der Bergstrasse, Germany)》2014,20(33):10249-10254
The intramolecular carbolithiation of a series of chloro‐substituted alkynes leads to exocyclic alkylidene carbenoids of which both nucleophilic and electrophilic characters can be drove. A sole stereoselective 5‐exo‐dig addition takes place, probably because of a strong and persisting Li–Cl interaction arising before the transition state. 相似文献
19.
《Journal of heterocyclic chemistry》2017,54(1):780-783
A small series of new 3,5‐dimethyl‐4‐(arylsulfanyl)pyrazoles have been synthesized in good to excellent yields by a grinding‐induced, sequential one‐pot three‐component reaction, of an equimolar mixture of 3‐chloro‐2,4‐pentanedione, differently substituted thiophenols, and hydrazine hydrate in the presence of piperidine under solvent‐free conditions. 相似文献
20.
The solvent effect on a nucleophilic substitution reaction of 2‐ and 4‐chloro‐3,5‐dinitrobenzotrifluoride with substituted anilines was studied in methanol, acetonitrile, and toluene at 25°C. This reaction is of second order, except 2‐chloro‐3,5‐dinitrobenzotrifluoride in toluene shows third order. The kA values are found to be dependent on the substituent in aniline and give good Hammett correlations. The obtained ρ values are ?4.07 and ?4.62, for the reaction of anilines with 2‐chloro‐3,5‐dinitrobenzotrifluoride in methanol and acetonitrile, respectively. The ρ values for the reaction of the anilines with 4‐chloro‐3,5‐dinitrobenzotrifluoride are ?3.38, ?4.11, and ?4.34 in methanol, acetonitrile, and toluene, respectively. The reaction of the former compound with anilines in toluene shows a second order in aniline. The dependence of the reaction on the external base such as DABCO suggests a proton transfer controlling step. © 2009 Wiley Periodicals, Inc. Int J Chem Kinet 41: 777–786, 2009 相似文献