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1.
Branko Stanovnik Uroš Urleb Miha Tišler 《Monatshefte für Chemie / Chemical Monthly》1987,118(5):601-606
An unequivocal synthesis of 5-chloro-7-methyl- (8) and 7-methyl-1,2,4-triazolo[1,5-a]pyrimidine (10) from 2-amino-4-chloro-6-methylpyrimidine (5) through the corresponding amidine6 and formamide oxime7 was developed. It was unambigously shown by comparison of the chemical shifts and the magnitude of coupling constants that the compounds obtained by condensation of 3-amino-1,2,4-triazole (12) and ethyl acetoacetate (13) and some further transformations are isomeric 5-methyl substituted 1,2,4-triazolo[1,5-a]pyrimidines1,9, and11.
Eine eindeutige Synthese einiger substituierter 1,2,4-Triazolo[1,5-a]pyrimidine
Zusammenfassung Es wurde ein eindeutiger Syntheseweg für 5-Chlor-7-methyl- (8) und 7-Methyl-1,2,4-triazolo[1,5-a]pyrimidin (10) ausgehend von 2-Amino-4-chlor-6-methylpyrimidin (5) über das entsprechende Amidin6 und das Formamidoxim7 entwickelt. Durch Vergleich von chemischen Verschiebungen und Kopplungskonstanten konnte eindeutig gezeigt werden, daß die Verbindungen, die bei der Kondensation von 3-Amino-1,2,4-triazol (12) and Ethylacetoacetat (13), sowie einige weitere Transformationsprodukte, isomere 5-Methylsubstituierte 1,2,4-Triazolo[1,5-a]pyrimidine sind (1,9,11).相似文献
2.
The syntheses of methyl 4‐(4‐nitrophenyl)‐3‐oxomorpholine‐2‐carboxylate ( 3a ) and ethyl 4‐(4‐nitrophenyl)‐2‐oxomorpholine‐3‐carboxylate ( 5b ), important building blocks for the synthesis of factor Xa inhibitor rivaroxaban analogs with potential dual antithrombotic activity, via Rh2(OAc)4‐catalyzed O? H and N? H carbene insertion reactions are described. 相似文献
3.
Gorazd Hribar Andrej Žnidaršič Marjan Bele Uroš Maver Simon Caserman Miran Gaberšček Vladka Gaberc-Porekar 《Journal of nanoparticle research》2011,13(7):3019-3032
The authors’ intention was to prepare nanometer-sized zinc-phosphate nanoparticles that would be capable of binding histidine-rich
TNF-α analogs onto their surface via a coordinative bond. Zinc-phosphate nanoparticles with a size of around 60 nm were prepared
by a wet precipitation method and characterized using SEM, EDX, XRD, and DLS. First, BSA was bound as a testing protein, afterward
two TNF-α analogs with decreased activity were bound to the described nanoparticles. The efficiency of binding and the existence
of coordinative bond were confirmed with SDS-PAGE analysis. During binding, particle storage, and release experiments, the
prepared TNF-α analogs retained their biological activity—hence the epitopes necessary for formation of antibodies stayed
intact. The particle size did not change within a period of 2 weeks. No significant agglomeration was observed, the particles
could be quickly dispersed in ultrasound. The present nanoparticles and the general approach of coordinative binding are widely
applicable for natural and engineered histidine-rich proteins. The nanoparticles bearing appropriate TNF-α analogs could also
be potentially used for active immunotherapy to tackle the chronic inflammatory diseases associated with pathogenically elevated
levels of TNF-α. 相似文献
4.
George Cordoyiannis Patricia Losada-Pérez Chandra Shekhar Pati Tripathi Brigita Rožič Uroš Tkalec Vassilios Tzitzios 《Liquid crystals》2013,40(11):1419-1426
The phase transition behaviour of the chiral liquid crystal CE6 doped with spherical surface-functionalised CdSe nanoparticles has been examined by means of high-resolution adiabatic scanning calorimetry and polarising microscopy. The addition of nanoparticles results in an essentially stabilised blue phase III. The phase diagram is displayed upon heating and cooling and the enthalpy changes involved in the conversion between the blue phases are determined. The dispersion of functionalised nanoparticles is prominent for the stabilisation of blue phase III, which is potentially useful for applications, especially if applied on liquid crystals that exhibit blue phases close to room temperature. 相似文献
5.
Uroš Grošelj Dieter Seebach D. Michael Badine W. Bernd Schweizer Albert K. Beck Ingo Krossing Petra Klose Yujiro Hayashi Tadafumi Uchimaru 《Helvetica chimica acta》2009,92(7):1225-1259
Structures of the reactive intermediates (enamines and iminium ions) of organocatalysis with diarylprolinol derivatives have been determined. To this end, diarylprolinol methyl and silyl ethers, 1 , and aldehydes, Ph? CH2? CHO, tBu? CH2? CHO, Ph? CH=CH? CHO, are condensed to the corresponding enamines, A and 3 (Scheme 2), and cinnamoylidene iminium salts, B and 4 (Scheme 3). These are isolated and fully characterized by melting/decomposition points, [α]D, elemental analysis, IR and NMR spectroscopy, and high‐resolution mass spectrometry (HR‐MS). Salts with BF4, PF6, SbF6, and the weakly coordinating Al[OC(CF3)3]4 anion were prepared. X‐Ray crystal structures of an enamine and of six iminium salts have been obtained and are described herein (Figs. 2 and 4–8, and Tables 2 and 7) and in a previous preliminary communication (Helv. Chim. Acta 2008 , 91, 1999). According to the NMR spectra (in CDCl3, (D6)DMSO, (D6)acetone, or CD3OD; Table 1), the major isomers 4 of the iminium salts have (E)‐configuration of the exocyclic N?C(1′) bond, but there are up to 11% of the (Z)‐isomer present in these solutions (Fig. 1). In all crystal structures, the iminium ions have (E)‐configuration, and the conformation around the exocyclic N‐C? C‐O bond is synclinal‐exo (cf. C and L ), with one of the phenyl groups over the pyrrolidine ring, and the RO group over the π‐system. One of the meta‐substituents (Me in 4b , CF3 in 4c and 4e ) on a 3,5‐disubstituted phenyl group is also located in the space above the π‐system. DFT Calculations at various levels of theory (Tables 3–6) confirm that the experimentally determined structures (cf. Fig. 10) are by far (up to 8.3 kcal/mol) the most stable ones. Implications of the results with respect to the mechanism of organocatalysis by diarylprolinol derivatives are discussed. 相似文献
6.
Uroš Todorović Dr. R. Martin Romero Dr. Lucile Anthore-Dalion 《European journal of organic chemistry》2023,26(31):e202300391
N−O σ bonds containing compounds are versatile substrates for organic synthesis under transition metal catalysis. Their ability to react through both polar (oxidative addition, formation of metallanitrene, nucleophilic substitution) and radical pathways (single electron transfer, homolytic bond scission) have triggered the development of various synthetic methodologies, particularly toward synthesizing nitrogen-containing compounds. In this review, we discuss the different modes of activation of N−O bonds in the presence of transition metal catalysts, emphasizing the experimental and computational mechanistic proofs in the literature to help to design new synthetic pathways toward the synthesis of C−N bonds. 相似文献
7.
Zakrajšek Srečko Rajkovič Vladislav Bernik Mojca Jereb Eva Rajkovič Uroš 《Central European Journal of Operations Research》2021,29(3):841-857
Central European Journal of Operations Research - Digital competences are among the most important competences in modern society, with the education system playing a key role in the acquisition of... 相似文献
8.
David Bevk Uroš Grošelj Anton Meden Jurij Svete Branko Stanovnik 《Helvetica chimica acta》2007,90(9):1737-1744
A simple and efficient synthesis of four new substituted pyrimidines, compounds 9a – d , from the title compound 3 is described. Conversion of 3 to methyl (E)‐3‐(dimethylamino)‐2‐(6‐methoxy‐2‐phenylpyrimidin‐4‐yl)prop‐2‐enoate ( 4 ), followed by condensation with various dinucleophiles according to the ‘enaminone methodology’, afforded the target compounds 9 in medium‐to‐good yields. 相似文献
9.
Simple Explicit Formulas for the Frame-Stewart Numbers 总被引:1,自引:0,他引:1
Several different approaches to the multi-peg Tower of Hanoi problem are equivalent. One of them is Stewart's recursive formula ¶¶ S (n, p) = min {2S (n1, p) + S (n-n1, p-1) | n1, n-n1 ? \mathbbZ+}. S (n, p) = min \{2S (n_1, p) + S (n-n_1, p-1)\mid n_1, n-n_1 \in \mathbb{Z}^+\}. ¶¶In the present paper we significantly simplify the explicit calculation of the Frame-Stewart's numbers S(n, p) and give a short proof of the domain theorem that describes the set of all pairs (n, n1), such that the above minima are achieved at n1. 相似文献
10.