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1.
The potassium salt of E- and Z-2,3-diphenylpropenoic acids prepared in situ could be esterified efficiently in DMSO with the appropriate alkyl halides at room temperature. In this way 10 previously undescribed esters of these acids were synthesised and characterised. Excellent yields were observed for most of the E isomers and the more hindered Z esters were also obtained in good yields, far better than those obtained applying the classical acid-catalysed esterification reaction. 相似文献
2.
Kaldor I Feldman PL Mook RA Ray JA Samano V Sefler AM Thompson JB Travis BR Boros EE 《The Journal of organic chemistry》2001,66(10):3495-3501
The quaternizations of dibenzoquinolizines 9 and 14 with 3-halo-1-propanols are highly cis-selective (94-100% cis), results consistent with the N-methylation of O-methylcapaurine (7b), but in contrast to the proposed trans-stereochemistry of dibenzo[a,h]quinolizine methiodide 10 and the analogous quaternizations of 1-benzyl- and 1-phenylisoquinoline congeners 5b and 5c. In this report, we describe stereoselective preparation of the unique cis-dibenzoquinolizinium propanols 15 and 16and their transformation into bis- and mixed-onium chlorofumarates 19, 20ab, and 26. Dibenzo[a,g]quinolizinium propanol 15 was prepared enantioselectively in three steps from dihydroisoquinoline 11. Asymmetric transfer hydrogenation of 11 in the presence of triethylamine/formic acid and Noyori's chiral ruthenium catalyst 12 produced R-(-)-5',8-dimethoxynorlaudanosine (13) in 98% yield and 87% ee. Pictet-Spengler cyclization of 13 in formalin/formic acid afforded the dibenzo[a,g]quinolizine 14 in 65% yield. Quaternization of 14 with 3-chloro-1-propanol under Finkelstein conditions generated cis-dibenzoquinolizinium propanol 15 in 85% yield with >94% cis-selectivity. The cis-dibenzo[a,h]quinolizinium propanol 16 was obtained as a single stereoisomer by reaction of the known tetramethoxyquinolizine 9 with neat 3-iodo-1-propanol. Bis-onium chlorofumarates 18 and 19 and the mixed-onium derivative 20ab were prepared by a pool synthesis procedure from (1R)-trans-6a, 16, and chlorofumaryl chloride (17). Mixed-onium alpha-chlorofumarate 26 was synthesized from (1S)-trans-6d, 15 and (+/-)-trans-2,3-dichlorosuccinic anhydride (22), employing a recently disclosed chlorofumarate mixed-diester synthesis. The title compounds (19, 20ab, and 26) displayed curare-like effects of ultrashort duration in rhesus monkeys. 相似文献
3.
Magda Mrton-Mersz Erzsbet Zra-Kaczin Sndor Boros Pter Mtyus 《Journal of heterocyclic chemistry》1997,34(3):1033-1036
Reaction of 2-acetonyl-4,5-dimethoxy-3′-chlorobenzophenone (1) with ethylenediamine afforded the imidazo[2,1-a]isoquinoline 2, whereas 6-(3-chlorophenyl)-8,9-dimethoxybenzo[b]phenazine (3) and naphthol 4 were obtained with ortho-phenylenediamine. 相似文献
4.
Summary Pressure and temperature have significant influence on retention in HPLC. This study investigates the effect of pressure and
temperature on the retention behavior of aromatic hydrocarbons (toluene, ethyl benzene, butyl benzene, pentyl benzene) and
polar, acidic and basic samples (phenol, acetophenone, N,N-dimethyl aniline, benzophenone) on a reversed phase column. The
effect has been studied on non-porous, tetradecyl (C14) coated silica particles. We found that the adsorption-induced decrease of the partial molar volume of the solutes investigated
was between ΔV
m
=5–15 cm3 mol−1. The increment of the decrease of the partial molar volume due to the addition of one CH2 group, for the homologous series of the aromatic hydrocarbons is approximately ΔV
CH2
=2.3 cm3mol−1.
Presented at Balaton Symposium '01 on High-Performance Separation Methods, Siófok, Hungary, September 2–4, 2001. 相似文献
5.
Endre Boros Khaled Elbassioni Vladimir Gurvich Leonid Khachiyan 《Mathematical Programming》2003,98(1-3):355-368
A result of Balas and Yu (1989) states that the number of maximal independent sets of a graph G is at most p+1, where is the number of pairs of vertices in G at distance 2, and p is the cardinality of a maximum induced matching in G. In this paper, we give an analogue of this result for hypergraphs and, more generally, for subsets of vectors in the product of n lattices =1××n, where the notion of an induced matching in G is replaced by a certain binary tree each internal node of which is mapped into . We show that our bounds may be nearly sharp for arbitrarily large hypergraphs and lattices. As an application, we prove that the number of maximal infeasible vectors x=1××n for a system of polymatroid inequalities does not exceed max{Q,logt/c(2Q,)}, where is the number of minimal feasible vectors for the system, , , and c(,) is the unique positive root of the equation 2c(c/log–1)=1. This bound is nearly sharp for the Boolean case ={0,1}n, and it allows for the efficient generation of all minimal feasible sets to a given system of polymatroid inequalities with quasi-polynomially bounded right-hand sides .
This research was supported by the National Science Foundation (Grant IIS-0118635), and by the Office of Naval Research (Grant N00014-92-J-1375). The second and third authors are also grateful for the partial support by DIMACS, the National Science Foundation's Center for Discrete Mathematics and Theoretical Computer Science.Mathematics Subject Classification (2000):20E28, 20G40, 20C20 相似文献
6.
We consider quadratic functions f that satisfy the additional equation y2 f(x) = x2 f(y) for the pairs \({ (x,y) \in \mathbb{R}^2}\) that fulfill the condition P(x, y) = 0 for some fixed polynomial P of two variables. If P(x, y) = ax + by + c with \({ a , b , c \in \mathbb{R}}\) and \({(a^2 + b^2)c \neq 0}\) or P(x,y) = x n ? y with a natural number \({n \geq 2}\), we prove that f(x) = f(1) x2 for all \({x \in \mathbb{R}}\). Some related problems, admitting quadratic functions generated by derivations, are considered as well. 相似文献
7.
Endre Boros 《Discrete Mathematics》2009,309(12):3853-321
Given a family of graphs , a graph is called edge-minimal (vertex-minimal) if for every subgraph (induced subgraph) G′ of G; furthermore, G is called locally edge-minimal (locally vertex-minimal) if whenever G′ is obtained from G by deleting an edge (a vertex). Similarly, the concepts of minimality and local minimality are introduced for directed graphs (digraphs) and, more generally, for partially ordered sets.For example, by the Strong Perfect Graph Theorem, the only vertex-minimal graphs with χ>ω are odd holes and anti-holes. In contrast, the only locally vertex-minimal graphs with χ>ω are partitionable graphs. Somewhat surprisingly, there are infinitely many non-trivial perfect graphs that are locally edge-minimal and -maximal simultaneously. In other words, such a graph is perfect but it becomes imperfect after any edge is deleted from or added to it.In this paper we consider vertex- and edge-minimal and locally minimal graphs in the following families: (i) perfect and imperfect graphs, (ii) graphs with χ=ω and with χ>ω, (iii) digraphs that have a kernel and kernel-free digraphs, and finally, (iv) vertex-minimal complementary connected d-graphs. 相似文献
8.
Eric E. Boros Istvan Kaldor Philip S. Turnbull 《Journal of heterocyclic chemistry》2011,48(3):733-736
2‐Methyl‐4‐(trifluoromethyl)‐1H‐indole‐5‐carbonitrile is a key intermediate in the synthesis of selective androgen receptor modulators discovered in these laboratories. A practical and convergent synthesis of the title compound starting from 4‐nitro‐3‐(trifluoromethyl)phenol and tert‐butyl acetoacetate was developed, including a telescoped procedure for synthesis (without isolation) and Nenitzescu reaction of 2‐trifluoromethyl‐1,4‐benzoquinone. Conversion of the known Nenitzescu indole product to a novel triflate intermediate followed by palladium‐catalyzed cyanation afforded a penultimate carbonitrile. Removal of the C‐3 tert‐butyl ester group on the indole through a decarboxylative pathway completed the synthesis of the title compound in six steps (27% overall yield) from 4‐nitro‐3‐(trifluoromethyl)phenol (five steps, 37% overall yield from tert‐butyl acetoacetate). J. Heterocyclic Chem., (2011). 相似文献
9.
Eric E. Boros James B. Thompson Edgar R. Wood O. Bradley McDonald Timothy D. Spitzer Andrea M. Sefler Bryan R. Reep 《Journal of heterocyclic chemistry》2004,41(3):355-358
5‐Methoxy and 5‐anilinopyrido[2,3‐d]pyrimidin‐7(8H)‐ones 2a‐2f were obtained by a tandem Michael addition‐cyclization reaction of methanol and anilines with pyrimidinylpropynoate 5. Methoxy derivative 2a was obtained in 62% yield by treatment of 5 with methanol and potassium carbonate. Anilino derivatives 2b‐2f were prepared in 31–71% yields by reacting 5 with the corresponding anilines in refluxing methanol. This methodology accomplishes Michael‐addition and pyridopyrimidinone ring formation in one‐pot and affords the desired products in reasonable yield without chromatography. Propynoate 5 did not react with 4‐cyanoaniline under these conditions. Reaction of 5 with 2‐aminopyridine gave the unexpected arylpyrido[2,3‐d]pyrimidinone 8 in 58% yield and reaction of 5 with imidazole afforded Michael‐adduct 9 in 69% yield. Compounds 2a and 5 were submicromolar inhibitors of epidermal growth factor receptor (EGFR) tyrosine kinase. 相似文献
10.
We point out that the component of the nucleon wave function is vital to the interpretation of the recent H1 data for leading baryon production.
While the n/p ratio is equal to two with the component alone, the inclusion of the component brings this ratio very near to unity, as observed in the experiment. This result demonstrates that pion exchange
can not only account for leading neutron but also for a large fraction of the leading proton production.
Received: 4 December 1998 / Revised version: 1 February 1999 / Published online: 27 April 1999 相似文献