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61.
Recent advances in the synthesis of C-5-substituted analogs of 3,4-dihydropyrimidin-2-ones: A review
3,4-Dihydropyrimidin-2-ones act as a versatile scaffold in organic synthesis, which serves as a significant template for the development of various therapeutic agents and shows a wide spectrum of activities. The attractive application of 3,4-dihydropyrimidin-2-ones in organic synthesis is undoubtedly owing to C-5 ester group, which is responsible for the change in its bioactivity. Introduction of various groups like electron-withdrawing and electron-donating groups at positions 1, 2, 3, 5, and 6 greatly increased biological activity. Significant efforts have been undertaken to exploit different synthetic routes to synthesize various derivatives of 3,4-dihydropyrimidin-2-ones. This review article gives a comprehensive account of the synthetic utility of C-5 substitution of 3,4-dihydropyrimidin-2-ones used in the design and synthesis of different types of compounds with greater emphasis on recent literature. 相似文献
62.
Kumar S Jain SK Rastogi RC 《Spectrochimica acta. Part A, Molecular and biomolecular spectroscopy》2001,57(2):291-298
The electronic absorption and fluorescence spectra of some biologically active natural flavones have been recorded at room temperature (298 K) in solvents of different polarities. The effects of the solvents upon the spectral properties are discussed. Difference in fluorescence intensity of flavones has been explained on the basis of intersystem crossing and degree of non-planarity calculated theoretically using Austin Model 1 (AM1) method. Excited-state dipole moments have been determined using the solvatochromic method based on the microscopic solvent polarity parameter, E(N)(T). A reasonable agreement has been observed between experimental and AM1 calculated dipole moment changes. Our results are found to be quite reliable in view of the fact that the correlation of the solvatochromic Stokes shifts with microscopic solvent polarity parameter, E(N)(T) is superior to that obtained using bulk solvent polarity functions for all the systems studied here. 相似文献
63.
Liquid chromatography was used for the quantification of aflatoxin B1-oxime (AFB1-oxime). The yield of AFB1-oxime in the reaction mixture was 89%, while after purification on silica gel it was 72%. LC analysis of the reaction mixture after silica gel fractionation revealed a retention time of 0.84 min for AFB1-oxime, 8.42 min for AFB1, 1.21 min for unknown 1 and 1.61 min for unknown 2. UV-visible analysis of the reaction mixture after silica gel fractionation showed a lambda(max) of 269 and 361 nm for AFB1-oxime, 263 and 360 nm for AFB1, 273 nm for unknown 1 and 275 nm for unknown 2. Excitation and emission wavelengths were found to be 269 and 368/438 nm for AFB1-oxime, 359/424 nm for AFB1, 270 and 367/450 nm for unknown 1 and 273 and 416/447 nm for unknown 2. The method may find versatile application in monitoring reactions for the preparation of oximes of various analytes for the synthesis of their immunogens. 相似文献
64.
Subphase conditions have been optimized to obtain stable organophosphorous hydrolase (OPH-EC 3.1.8.1) as Langmuir films. The Langmuir film was characterized by surface pressure and surface potential-area isotherms and UV-Vis spectroscopy in situ. The interaction of an organophosphorous compound, namely Paraoxon, with the OPH film was investigated for various surface pressures. The stability of the monolayer and the evidence of the enzyme activity at air-water interface support the use of enzyme LB films as biosensor. 相似文献
65.
Tripathi RP Rastogi SK Kundu B Saxena JK Reddy VJ Srivastava S Chandra S Bhaduri AP 《Combinatorial chemistry & high throughput screening》2001,4(3):237-244
A library of 24 glycoconjugates related to glycosylated beta-amino acid derivative (I) was been prepared and screened against DNA topoisomerase-II of the filarial parasite S. cervi. Among these, compound 6 was found to be a potent inhibitor of DNA topoisomerase-II with 95% inhibition at 1.09 microM. Furthermore, compound 6 was at least three times more potent than the lead compound, glycosylated beta-amino acid derivative I. 相似文献
66.
Sanjay Kumar Ankur Jain Yoshitsugu Kojima 《Journal of Thermal Analysis and Calorimetry》2017,128(2):721-733
This paper studies the addition (0–40% w/w) of natural zeolite (NZ, 84% clinoptilolite) in blended cements made with Portland cement (PC) with low and medium C3A content. The isothermal calorimetry was used to understand the effect of NZ on the early cement hydration. For low C3A cement, the addition of NZ produces mainly a dilution effect and then the heat released curve is similar to plain cement with lower intensity. For medium C3A cement, the curve shows the C3S peak in advance and a high intensity of third peak attributed to C3A hydration. The high cation fixed of NZ reduces the ions concentration (especially alkalis) in the mixing water stimulating the PC hydration. The flowability decreases when the NZ replacement level increases. Results of Fratini’s test show that NZ with both PCs used presents slow pozzolanic activity. At early age, XRD and FTIR analyses confirm that hydration products are the same as that of the corresponding PC and the CH is progressively reduced after 28 days and some AFm phases (hemi- and monocarboaluminate) appear depending on the NZ percentage and the PC used. For low replacement levels, the compressive strength is higher than the corresponding PC from 2 to 28 days. For high replacement levels, the early compressive strength is lower than that of corresponding plain PC and the pozzolanic reaction improves the later compressive strength of blended cements. 相似文献
67.
Coplanar waveguides (CPW) used in microwave integrated circuits are significantly dispersive. An analytical approximation to the frequency dependence of both eff and c of CPW with finite metallisation thickness and conductivity is discussed. The effect of increasing loss tangent on dielectric constant is also presented. 相似文献
68.
The body of knowledge necessary to observe holographic-moiré patterns in real time is introduced. The basic factors influencing fringe visibility in holographic moiré are analyzed and expressions to evaluate fringe visibility for any given displacement and deformation are given. The application of the introduced theory in the case of real-time observation is discussed. It is shown that the maximum benefits of this technique are achieved by combining it with closed-circuit TV. Several examples of application are given. 相似文献
69.
A maximum-likelihood (ML) method based on spectral estimation theory for the extraction of dual phase distributions in holographic moire in the presence of nonsinusoidal waveforms, noise, and the miscalibration of piezoelectric (PZT) devices is proposed. The extraction of these phases requires incorporating two PZTs into the moire setup. ML estimators are asymptotically efficient for sufficient data samples. The approach presented uses a direct stochastic algorithm called probabilistic global search Lausanne for minimizing the ML function. 相似文献
70.
Metal-oxide-semiconductor (MOS) storage capacitors based on electron beam deposited Y2O3 extrinsic dielectric on Si show changes in capacitance density depending on the amorphous and crystalline phases. Bias stress
cycle-dependent changes in capacitance density occur due to the non-equilibrium nature of defect states at the Y2O3/Si interface after O2 annealing as a result of the emergence of a 4–8 nm thick SiO2 film at the interface. Leakage currents show instability under repeated dc bias stress, the nature and extent of which depend
upon the structure of the Y2O3 gate dielectric and the polarity of dc bias. With amorphous Y2O3, leakage currents drift to lower values under gate injection due to electron trapping, and to higher values under Si-injection
due to the generation of holes. Though leakage current drift is minimal for crystalline Y2O3, its magnitude increases as the energy of injected electrons from mid-gap states is low and the local field due to asperity
is high. The emergence of interfacial SiO2 reduces the magnitude of Si-injection leakage current substantially, but causes transient changes resulting in switching
to higher values at a threshold dc bias. Thermal detrapping of holes and reverse bias stress studies confirm that the instability
of current is caused by an increase in the cathodic field from hole trapping at interface states. Leakage current instability
limits the application of extrinsic high dielectric constant dielectrics in a high density DRAM storage capacitor, unless
a new interface layer scheme other than SiO2 and a method to form a defect-free dielectric layer can be implemented.
Received: 29 October 2001 / Accepted: 22 April 2002 / Published online: 4 December 2002
RID="*"
ID="*"Corresponding author. Fax: +1-413/545-4611, E-mail: rastogi@ecs.umass.edu 相似文献