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A facile and efficient synthesis of 1,5‐benzodiazepines with an arylsulfonamido substituent at C(3) is described. 1,5‐Benzodiazepine, derived from the condensation of benzene‐1,2‐diamine and diketene, reacts with an arylsulfonyl isocyanate via an enamine intermediate to produce the title compounds of potential synthetic and pharmacological interest in good yields (Scheme 1). In addition, reaction of benzene‐1,2‐diamine and diketene in the presence of benzoyl isothiocyanate leads to N‐[2‐(3‐benzoylthioureido)aryl]‐3‐oxobutanamide derivatives (Scheme 2). This reaction proceeds via an imine intermediate and ring opening of diazepine. The structures were corroborated spectroscopically (IR, 1H‐ and 13C‐NMR, and EI‐MS) and by elemental analyses. A plausible mechanism for this type of cyclization is proposed (Scheme 3). 相似文献
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Optimization Letters - In the original publication of the article, the name of the corresponding author was incorrectly published as “Amir Ahamdi”. 相似文献
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The one-pot synthesis of 2,3-dihydro-1,5-benzodiazepins-2-one bearing phosphanylidene (ylide) or phosphono-succinate substituent is described. In this four-component reaction, benzodiazepine derived from condensation of o-phenylenediamine and diketene is trapped with the trialkyl phosphite-dialkyl acetylenedicarboxylate zwitterion. In the presence of H2O, the ylide functional group is hydrolyzed to the corresponding phosphonate. The configuration of the products is selective and only one of the two possible rotamers or diastereomers is formed exclusively in high yield. 相似文献
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Multiple criteria facility location problems: A survey 总被引:1,自引:0,他引:1
This paper provides a review on recent efforts and development in multi-criteria location problems in three categories including bi-objective, multi-objective and multi-attribute problems and their solution methods. Also, it provides an overview on various criteria used. While there are a few chapters or sections in different location books related to this topic, we have not seen any comprehensive review papers or book chapter that can cover it. We believe this paper can be used as a complementary and updated version. 相似文献
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Chromium trioxide/periodic acid supported onto wet silica gel oxidizes primary alcohols to the corresponding carboxylic acids in very short reaction times in very good yields. 相似文献
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Davood Nori‐Shargh Abolfazl Soofi Nasrin Saroogh Farahani Farzad Deyhimi 《国际化学动力学杂志》2005,37(7):427-433
This work reports the results of a kinetic and mechanistic investigations of the addition reaction of triphenylphosphine to para‐naphtoquinone in 1,2‐dichloromethane as solvent. The order of reaction with respect to the reactants was determined using initial rate method, and the rate constant was obtained on the basis of pseudo‐first‐order method. Variable time method using Uv–Vis spectrophotometry (at 400 nm) was utilized for monitoring this addition reaction, for which the following Arrhenius equation was obtained: The resulting activation parameters Ea, ΔH#, ΔG#, and ΔS# at 300 K were 13.63, 14.42, 18.75 kcal mol?1, and ?14.54 cal mol?1K?1, respectively. The results suggest that the reaction is first order with respect to both triphenylphosphine and para‐naphthoquinone. © 2005 Wiley Periodicals, Inc. Int J Chem Kinet 37: 427–433, 2005 相似文献
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Four new monomeric Pd (II) complexes with formulas [Pd(C,N)‐(2′‐NH2C6H4)C6H4 (N3)(L)] ( A ), ( B ) and [Pd(C,N)‐C6H4CH2NH(C4H9)(N3)(L)] ( C ), ( D ), [L = isonicotinamide for ( A ) and ( C ), L = 4‐N,N‐dimethylaminopyridine for ( B ) and ( D )] have been synthesized using four initial dimers [Pd2{(C,N)‐(2′‐NH2C6H4)C6H4}2(μ‐OAc)2] ( 1 ), [Pd2{(C,N)‐ (2′‐NH2C6H4)C6H4}2(μ‐N3)2] ( 3 ) for A and C , and [Pd2{(C,N)‐C6H4CH2NH(C4H9)}2(μ‐OAc)2] ( 2 ) and [Pd2{(C,N)‐C6H4CH2NH(C4H9)}2(μ‐N3)2] ( 4 ) for B and D . Then synthesized complexes have been characterized by Fourier transform‐infrared, NMR spectroscopy and thermal gravimetric‐differential thermal analysis. Furthermore, UV–Vis spectroscopy, fluorescence spectroscopy, circular dichroism (CD) and helix melting temperature measurements have been employed to study the binding interaction of them with calf thymus‐deoxyribonucleic acid (DNA). The results reveal that all synthesized complexes can interact with DNA via groove‐binding mode. Bovine serum albumin (BSA)‐binding studies have been carried out using UV–Vis spectroscopy, emission titration and CD. However, competitive binding studies using warfarin, ibuprofen and digoxin on site markers demonstrated that the complexes bind to different sites on BSA. The results also indicated that the binding site was mainly located within site‐III for complex A , and site‐I for complexes B , C and D of BSA. In addition, molecular docking studies have been executed to determine the binding site of the DNA and BSA with complexes. Eventually, in vitro cytotoxicity of synthesized palladium complexes and cisplatin were carried out against human promyelocytic leukemia cancer (Hela) and breast cancer (MCF‐7) cell lines. Pursuant to the IC50 values, the cytotoxicity of complexes against MCF‐7 was more than Hela. 相似文献