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1.
The complex natural product paclitaxel (Taxol,la), first isolated from Taxus brevifolia,has an excellent clinical activity against ovarian and breast cancers and shows promising results in the treatment of other cancers. The structureactivity relationships (SAR) of taxoid derivatives have been extensively studied to search for the analogues bearing better physical, chemical and biological properties. One example is the discovery of  相似文献   

2.
PaclitaxelisapromisinganticancerdmgusedfortreatInentofbreastandovarycancer.lSARstUdieshaverevealedthatthefunctionalitiesatthes0uthemhemisphereofthemoleculeareimPortantf0rantitUmoractivity',butl-hydroXyisstillablackb0x.TwogrouPs"shaveindePendentlyremovedC-l0oxygenfunctionalityusingsamariumdiiodide,anelectrontransferlanthanidereagent,stedingfr0mbaccatinIIIorfr0mpaclitaxel.Wereasonedthatthel-OHofbaccatinlllmightberemovedbyfirstconvertingC-2benzoateint0aketone,whichwillreducethesterichindran…  相似文献   

3.
IntroductionSince C. W. Tang firstly reported theelectroluminescence of 8- hydroxyquinolinealuminium[1] ,much attention has been paid to themetal complexes as electro- luminescent materials.Based on a series of experimental data,it has beenknown that the electroluminescence of metalcomplexes with heterocyclic ligands containing Nand O elements mainly results from the tripletstatetransition.For some transitional metal complexes,there exist the transitions from metal to ligand( MLCT) at thei…  相似文献   

4.
A simple route for the preparation of lipo-alkaloid is presented. When aconitine or one of its analogues is heated with a fatty acid for 20 min at 100℃ in water, the C8 acetyl group of aconitine is displaced by a long chain fatty acyl group. The structures of the products were characterized by electrospray ionization tandem mass spectrometry.  相似文献   

5.
1-(α-Aminomethyl)-1,2,4-triazoles readily add to enol ethers or enamides to give novel classes of compounds, 1-(γ-amino-α-alkoxy)propyl- (8) and 1-(γ-amino-α-amido)propyl- (10) substituted 1,2,4-triazoles, in excellent yields.  相似文献   

6.
We describe a useful synthesis of a variety of β,β-bis(alkylthio)acrylonitriles via the alkylation of the salt arising from the condensation of acetonitrile with carbon disulfide in ether.  相似文献   

7.
IntroductionSince Tang[1] and Adachi et al.[2 ] reportedtheir double- and triple- layered devices,organicelectroluminescent(EL ) devices have attracted agreat interest due to their efficient emission in thevisible region and their possible application to flatpanel full color display.Among red- emissionorganic materials,europium complexes haveattracted researchers intense attention[3— 10 ]because the sharp emission band of Eu- complexeshas demonstrated the advantage of a very sharp ELemissio…  相似文献   

8.
Acid catalysed cyclization of citral to give α, p-dimethyl styrene using chloranil as an ozidizing agent is reported. The important aspect of this transformation is the dehydration of intermediate piperitenol followed by dehydrogenation to furnish the target compound in 80.5% yield.  相似文献   

9.
7-Hydroxyderivativesofcholesteroldisplayawidevarietyofbiologicalactivities'-',mostofwhicharerelatedtothephysiologicalcontrolofcholesterolbiosynthesisandantitumoractivity.Inearlyreports',the7-hydroxycholesterolswerepreparedbythesequenceofacetylation,allylicchromicoxidation,andhydridereduction.Generally,theproductisamixtureof7a-and76-epimerswhichisdifficulttobeseparated.V.Kumaretal5improvedthisprocedurebyusingstereospecificreducingreagentsinsteadofthesimplehydride.7a-and7o-epimerscouldbeobtained…  相似文献   

10.
It is emergent to develop a green waste water adsorbent with high efficiency.Therefore,a type of low-cost,green and environmentally friendly konjac glucomannan(KGM)-silk fibroin(SF)composite aerogels were compounded via simple chemical grafting and vacuum freeze drying,and a study on its adsorption capacity was also conducted.The characterizations of FT-IR,SEM,XRD and DSC indicate that the modified aerogels show a porous network space structure and there is a strong hydrogen bond effect between the KGM and SF molecules,which improves the density,compressive strength and thermal stability of aerogel materials.The adsorption experiments show that KGM-SF aerogels can effectively adsorb the water pollutants Cr(Ⅲ)with a maximal adsorption capacity of 82 mg·g-1.In addition,the adsorption isotherm and dynamic model analysis are used to elaborate the adsorption mechanism of KGM-SF aerogels and explain that the composite aerogels can be single molecule chemisorption.KGM-SF aerogels have potential adsorption capacity.  相似文献   

11.
The reaction of N-benzyl -amino acid ethyl esters with ethylmagnesium bromide in the presence of a catalytic amount of titanium tetraisopropoxide leads to formation of the corresponding 1-aminoalkyl- 1-cyclopropanols in high yields. Hydrogenation of the latter over palladium catalyst ensures selective removal of one or two protecting benzyl groups from the nitrogen atom.  相似文献   

12.
Several 3-benzylidenephthalides have been isolated from natural sources1-2. Some of them are known to possess useful biological activity1 and are also valuable intermediates3 for the synthesis of naturally occurring biologically active compound. Most of the natural 3-benzylidenephthalides exist in the (Z)-configuration. Synthe-tic methods for construction of a 3-benzylidene-phthalide skeleton have been developed4. Some of these methods for synthesizing highly oxygen-functionalized compound…  相似文献   

13.
A general and practical chemical route to the synthesis of N‐sulfonylimines using montmorillonite K‐10 as the catalyst is described. This method provides several advantages such as operational simplicity, short reaction time, using of inexpensive materials, noncorrosivity, lack of pollution, and high yields.  相似文献   

14.
A new La(Ⅲ) complex, {[La(L)(NO3)(H2O)3]·H2O}n (L = 1,10-phenanthroline- 2,9-dicarboxylate), has been synthesized and structurally determined by X-ray diffraction analysis. The complex crystallizes in the monoclinic system, space group P21/c with a = 7.7358(17), b = 8.1664(18), c = 28.271(6) , β = 95.184(4)°, V = 1778.6(7)3, Z = 4, C14H14LaN3O11, Mr = 539.19, Dc = 2.014 g/cm3, μ = 2.471 mm–1, F(000) = 1056, the final R = 0.0350 and wR = 0.0659. In this complex, each metal center adopts a ten-coordination geometry formed by two N atoms from a ligand L and eight O atoms from three H2O molecules, a nitrate ion and carboxylates of two ligands. Each ligand adopts a N2,O3-pentdentate coordination mode using two N and two O atoms chelating a La(III), and using another O atom of carboxylate to bridge another La(III) center resulting in a 1D helical chain molecule. Intermolecular strong O–H···O and weak C–H···O hydrogen bonds extend the 1D chain structure into a 3D supramolecular architecture.  相似文献   

15.
The present paper covers the synthesis and the characterization of ligand 2-decyl-3, 6, 9-tris(carboxymethyl)-3,6,9-triazaundecan-1,11-dioic acid, H5L, and its Gd(Ⅲ) chelate. The protonation constants for H5L(lgKHi=10.90, 8.50, 4.55, 2.92, 2.20) and the stability constant for GdL2- (lgKGdL2-=22.80) were determined by means of potentiometric titration. They are similar to the corresponding values of DTPA and Gd-DTPA, respectively. The results obtained show that the basicity of the ligand and the stability constant of its Gd(Ⅲ) chelate are not obviously altered after the introduction of a linear chain decyl group into the terminal acetic acid residue of DTPA. The Gd(Ⅲ) chelate may be a potential contrast agent with liver-specificity for magnetic resonance imaging(MRI).  相似文献   

16.
17.
Preparation of perchloric acid supported on alumina and its primary application as a solid supported heterogeneous catalyst to the synthesis of α-(α-amidobenzyl)-β-naphthols by a one-pot, three-component condensation of benzaldehydes, β-naphthol and acetamide or benzamide under thermal solvent-free conditions were described. The present methodology offers several advantages such as simple procedure, shorter reaction time, and excellent yields.  相似文献   

18.
A new, simple, environmentally friendly synthesis of dihydropyrimidinones from aromatic and aliphatic aldehydes, ethyl acetoacetate, and urea or thiourea using a small‐pore‐size zeolite as catalyst is described. Compared with the classical Biginelli reaction conditions, this method has the advantage of high yield, shorter reaction time, and recyclable and reusable catalyst.  相似文献   

19.
1 INTRODUCTION Macrocyclic ligands and their metal complexes have received much attention due to their applications in ion transport, ion separation and as models in biomimic researches[1~7]. The synthetic methods of macrocyclic ligands and their metal complexes are mainly divided into three kinds[8]. The first one is synthesizing free ligand, then forming the metal complexes; the second is template synthesis; and the third is synthesizing the end-off or side-off precursor ligand, then c…  相似文献   

20.
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