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51.
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Dawei Chen Ridao Chen Ruishan Wang Jianhua Li Kebo Xie Chuancai Bian Lili Sun Xiaolin Zhang Jimei Liu Lin Yang Fei Ye Xiaoming Yu Jungui Dai 《Angewandte Chemie (Weinheim an der Bergstrasse, Germany)》2015,127(43):12869-12873
The catalytic promiscuity of the novel benzophenone C‐glycosyltransferase, MiCGT, which is involved in the biosynthesis of mangiferin from Mangifera indica, was explored. MiCGT exhibited a robust capability to regio‐ and stereospecific C‐glycosylation of 35 structurally diverse druglike scaffolds and simple phenolics with UDP‐glucose, and also formed O‐ and N‐glycosides. Moreover, MiCGT was able to generate C‐xylosides with UDP‐xylose. The OGT‐reversibility of MiCGT was also exploited to generate C‐glucosides with simple sugar donor. Three aryl‐C‐glycosides exhibited potent SGLT2 inhibitory activities with IC50 values of 2.6×, 7.6×, and 7.6×10−7 M , respectively. These findings demonstrate for the first time the significant potential of an enzymatic approach to diversification through C‐glycosidation of bioactive natural and unnatural products in drug discovery. 相似文献
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A rigid supramolecular polymer was constructed in aqueous solution via cucurbit[8]uril(CB[8]) host recognition with a rigid monomer containing an azobenzene unit and two 4,4'-bipyridin-1-ium(BP)moieties in the two ends, which also exhibited photo-responsiveness owing to the photoinduced trans–cis isomerization of azobenzene group. 相似文献
55.
Back Cover: Reactions of Group 4 Metallocenes with Monosubstituted Acetonitriles: Keteniminate Formation versus CC Coupling (Chem. Eur. J. 8/2015) 下载免费PDF全文
56.
Prof. Antonio Molinaro Prof. Otto Holst Dr. Flaviana Di Lorenzo Dr. Maire Callaghan Dr. Alessandra Nurisso Dr. Gerardino D'Errico Dr. Alla Zamyatina Prof. Francesco Peri Dr. Rita Berisio Prof. Roman Jerala Prof. Jesús Jiménez‐Barbero Dr. Alba Silipo Prof. Sonsoles Martín‐Santamaría 《Chemistry (Weinheim an der Bergstrasse, Germany)》2015,21(2):500-519
In many Gram‐negative bacteria, lipopolysaccharide (LPS) and its lipid A moiety are pivotal for bacterial survival. Depending on its structure, lipid A carries the toxic properties of the LPS and acts as a potent elicitor of the host innate immune system via the Toll‐like receptor 4/myeloid differentiation factor 2 (TLR4/MD‐2) receptor complex. It often causes a wide variety of biological effects ranging from a remarkable enhancement of the resistance to the infection to an uncontrolled and massive immune response resulting in sepsis and septic shock. Since the bioactivity of lipid A is strongly influenced by its primary structure, a broad range of chemical syntheses of lipid A derivatives have made an enormous contribution to the characterization of lipid A bioactivity, providing novel pharmacological targets for the development of new biomedical therapies. Here, we describe and discuss the chemical aspects regarding lipid A and its role in innate immunity, from the (bio)synthesis, isolation and characterization to the molecular recognition at the atomic level. 相似文献
57.
Theoretical investigations on the insertion reaction mechanisms of three- membered-ring silylenoid H2 Si Li F with GeH 3R(R = F, OH, NH2) have been systematically carried out by combined density functional theory(DFT) and ab initio quantum chemical calculations. The geometries of all stationary points for these reactions were optimized using the B3 LYP method and then the QCISD method was used to calculate the single-point energies. The calculated results indicate that, there are one precursor complex(Q), one transition state(TS), and one intermediate(IM) which connect the reactants and the products along the potential energy surface. The insertion reactions of three-membered-ring silylenoid with Ge H3 R proceed in a concerted manner, forming H2RSi-Ge H3 and Li F. The calculated potential energy barriers of the three reactions are 29.17, 30.90, and 54.07 k J/mol, and the reaction energies for the three reactions are –127.05, –116.91, and –103.31 k J/mol, respectively. The insertion reactions in solvents are similar to those in vacuum. Under the same situation, the insertion reactions should occur easily in the following order: GeH 3-F GeH 3-OH GeH 3-NH2. The elucidations of the mechanism of these insertion reactions provided a new mode of silicon-germanium bond formation. 相似文献
58.
Palladium‐Catalyzed Domino CH/NH Functionalization: An Efficient Approach to Nitrogen‐Bridged Heteroacenes 下载免费PDF全文
Natsuyo Kamimoto Dr. Dieter Schollmeyer Dr. Koichi Mitsudo Prof.Dr. Seiji Suga Prof.Dr. Siegfried R. Waldvogel 《Chemistry (Weinheim an der Bergstrasse, Germany)》2015,21(22):8257-8261
Palladium‐catalyzed domino C?H/N?H functionalization for the synthesis of novel nitrogen‐bridged thienoacenes and 10H‐benzo[4,5]thieno[3,2‐b]indole derivatives from dihaloarene is reported. This domino sequence consists of initial C?H functionalization of the benzo[b]thiophene moiety, followed by Buchwald–Hartwig coupling. This transformation is also useful for the synthesis of highly π‐extended compounds. 相似文献
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Elham Tabrizian Ali Amoozadeh Salman Rahmani Elham Imanifar Saeede Azhari Masoumeh Malmir 《中国化学快报》2015,26(10):1278-1282
Nano titania-supported sulfonic acid (n-TSA) has found to be a highly efficient, eco-friendly and recyclable heterogeneous nanocatalyst for the solvent-free synthesis of 2, 4, 6-triarylpyridines through one-pot three-component reaction of acetophenones, aryl aldehydes and ammonium acetate. This reported method illustrates several advantages such as environmental friendliness reaction conditions, simplicity, short reaction time, easy work up, reusability of catalyst and high yields of the products. One new compound is reported too. Furthermore, the catalyst could be recycled after a simple work-up, and reused at least six times without substantial reduction in its catalytic activity. 相似文献