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81.
Gram‐Scale Enantioselective Formal Synthesis of Morphine through an ortho–para Oxidative Phenolic Coupling Strategy 下载免费PDF全文
Dr. Matthieu Tissot Dr. Robert J. Phipps Dr. Catherine Lucas Dr. Rafael M. Leon Dr. Robert D. M. Pace Dr. Tifelle Ngouansavanh Prof. Matthew J. Gaunt 《Angewandte Chemie (International ed. in English)》2014,53(49):13498-13501
A gram‐scale catalytic enantioselective formal synthesis of morphine is described. The key steps of the synthesis involve an ortho–para oxidative phenolic coupling and a highly diastereoselective “desymmetrization” of the resulting cyclohexadienone that generates three of the four morphinan ring junction stereocenters in one step. The stereochemistry is controlled from a single carbinol center installed through catalytic enantioselective hydrogenation. These transformations enabled the preparation of large quantities of key intermediates and could support a practical and scalable synthesis of morphine and related derivatives. 相似文献
82.
Dr. Xinghai Ning Dr. Wonewoo Seo Dr. Seungjun Lee Dr. Kiyoko Takemiya Dr. Mohammad Rafi Dr. Xuli Feng Dr. Daiana Weiss Dr. Xiaojian Wang Larry Williams Vernon M. Camp Malveaux Eugene Prof. W. Robert Taylor Prof. Mark Goodman Prof. Niren Murthy 《Angewandte Chemie (International ed. in English)》2014,53(51):14096-14101
A positron emission tomography (PET) tracer composed of 18F‐labeled maltohexaose (MH18F) can image bacteria in vivo with a sensitivity and specificity that are orders of magnitude higher than those of fluorodeoxyglucose (18FDG). MH18F can detect early‐stage infections composed of as few as 105 E. coli colony‐forming units (CFUs), and can identify drug resistance in bacteria in vivo. MH18F has the potential to improve the diagnosis of bacterial infections given its unique combination of high specificity and sensitivity for bacteria. 相似文献
83.
Violeta Benedetti-Doctorovich Fu-Yung Huang John Lambropoulos Edward M. Burgess Leon H. Zalkow 《合成通讯》2013,43(22):3701-3709
The aporphine alkaloid N-carbethoxydehydronorglaucine (1) was found to have promising in vitro antitumor activity, but poor water solubility. We report the synthesis of 1, the efficient hydrolysis of its urethane group and the further transformation into several new dehydronorglaucine analogs. 相似文献
84.
Morphine fluorescence spectra were obtained for morphine sulfate in distilled water, in KRP solution, and in KRP solutions with various concentrations of Ca++ and Mg++. No evidence of fluorescence shifting indicative of complex formation was observed. Similar solutions were used in a potentiometric study, and no evidence for complex formation was observed. 相似文献
85.
86.
Y. Leon P. Sciau P. Goudeau N. Tamura S. Webb A. Mehta 《Applied Physics A: Materials Science & Processing》2010,99(2):419-425
In addition to the red terra sigillata production, the largest Gallic workshop (La Graufesenque) made a special type of terra sigillata, called “marbled” by the archaeologists. Produced exclusively at this site, this pottery is characterized by a surface finish
made of a mixture of yellow and red slips. Because the two slips are intimately mixed, it is difficult to obtain the precise
composition of one of the two constituents without contamination from the other. In order to obtain very precise correlation
at the appropriate scale between the color aspect and the elemental and mineralogical phase distributions in the slip, combined
electron microprobe, X-ray micro spectroscopies and micro diffraction on cross-sectional samples were performed. The aim of
this study is to discover how potters were able to produce this unique type of terra sigillata and especially this particular slip of an intense yellow color. Results show that the yellow component of marbled sigillata was made from a titanium-rich clay preparation. The color is due to the formation of a pseudobrookite (TiFe2O5) phase in the yellow part of the slip, the main characteristics of that structure being considered nowadays as essential
for the fabrication of stable yellow ceramic pigments. Its physical properties such as high refractive indices and a melting
point higher than that of most silicates widely used as ceramic colorants are indeed determinant for this kind of application.
Finally, the red parts have a similar composition (elementary and mineralogical) to the one of standard red slip. 相似文献
87.
TREN (Tris(2-aminoethyl)amine): an effective scaffold for the assembly of triple helical collagen mimetic structures 总被引:1,自引:0,他引:1
Kwak J De Capua A Locardi E Goodman M 《Journal of the American Chemical Society》2002,124(47):14085-14091
A new scaffold, TREN-(suc-OH)(3) where TREN is tris(2-aminoethyl)amine and suc is the succinic acid spacers, was incorporated to assemble triple helices composed of Gly-Nleu-Pro sequences (Nleu denotes N-isobutylglycine). Extensive biophysical studies which include denaturation studies, CD and NMR spectroscopy, and molecular modeling demonstrated that TREN-[suc-(Gly-Nleu-Pro)(n)-NH(2)](3) (n = 5 and 6) form stable triple helical structures in solution. A comparative analysis of TREN-assembled and KTA-assembled collagen mimetics (KTA denotes Kemp triacid, 1,3,5-trimethylcyclohexane-1,3,5-tricarboxylic acid) indicates that the flexibility of the TREN scaffold is superior to the KTA scaffold in inducing triple helicity. This effect most likely arises from the flexibility of the TREN scaffold which allows the three peptide chains to adjust their register for a tighter triple helical packing. 相似文献
88.
[reaction: see text] The syntheses of 4,4a-didehydrohimbacine and 4,4a-didehydrohimandravine are presented. Key steps include an intramolecular Diels-Alder reaction of a bromopentadienyl acrylate and Suzuki-Miyaura and Stille coupling reactions. 相似文献
89.
As the coupling in a heterogeneous excitable medium is reduced, three different types of behavior are encountered: plane waves propagate without breaking up, plane waves break up into spiral waves, and plane waves block. We illustrate these phenomena in monolayers of chick embryonic heart cells using calcium sensitive fluorescent dyes. Following the addition of heptanol, an agent that reduces the electrical coupling between cells, we observe breakup of spiral waves. These results are modeled in a heterogeneous cellular automaton model in which the neighborhood of interaction is modified. 相似文献
90.
This paper serves as an introduction to the Focus Issue on mapping and control of complex cardiac arrhythmias. We first introduce basic concepts of cardiac electrophysiology and describe the main clinical methods being used to treat arrhythmia. We then provide a brief summary of the main themes contained in the articles in this Focus Issue. In recent years there have been important advances in the ability to map the spread of excitation in intact hearts and in laboratory settings. This work has been combined with simulations that use increasingly realistic geometry and physiology. Waves of excitation and contraction in the heart do not always propagate with constant velocity but are often subject to instabilities that may lead to fluctuations in velocity and cycle time. Such instabilities are often treated best in the context of simple one- or two-dimensional geometries. An understanding of the mechanisms of propagation and wave stability is leading to the implementation of different stimulation protocols in an effort to modify or eliminate abnormal rhythms. (c) 2002 American Institute of Physics. 相似文献