- The Role of Substituent Effects in Tuning Metallophilic Interactions and Emission Energy of Bis-4-(2-pyridyl)-1,2,3-triazolatoplatinum(II) Complexes
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The photoluminescence spectra of a series of 5-substituted pyridyl-1,2,3-triazolato PtII homoleptic complexes show weak emission tunability (ranging from λ=397-408 nm) in dilute (10-6 M) ethanolic solutions at the monomer level and strong tunability in concentrated solutions (10-4 M) and thin films (ranging from λ=487-625 nm) from dimeric excited states (excimers). The results of density functional calculations (PBE0) attribute this "turn-on" sensitivity and intensity in the excimer to strong Pt-Pt metallophilic interactions and a change in the excited-state character from singlet metal-to-ligand charge transfer (1MLCT) to singlet metal-metal-to-ligand charge transfer (1MMLCT) emissions in agreement with lifetime measurements. Turn-on tunability: A series of bis-4-(2-pyridyl)-1,2,3-triazolatoplatinum(II) complexes display variable emission tunability. At low concentration, the emission can be tuned only slightly by changing the nature of the substituent but at higher concentrations tunability is enhanced. This "turn-on" sensitivity in the excimeric emission is attributed to strong Pt-Pt metallophilic interactions and a change in the excited-state character.
- Prabhath, M. R. Ranga,Romanova, Julia,Curry, Richard J.,Silva, S. Ravi P.,Jarowski, Peter D.
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Read Online
- Synthesis of multitopic bidentate ligands based on alternating pyridine and pyridazine rings
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A synthetic route based on Stille coupling between tributyltinpyridyl derivatives and chloropyridazines is used for the synthesis of ditopic bidentate ligands 8, 9 and 10. This methodology can be extended for the synthesis of a linear tetradentate ligand 11 with four pyridine and two pyridazine rings.
- Romero-Salguero, Francisco Jose,Lehn, Jean-Marie
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Read Online
- Self-assembled porphyrin-based cage complexes, M11L6 (M = ZnII, CdII), with inner coordination sites in their crystal structure
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Herein we report self-assembled metallo-cage complexes, M11(L1)6 (M = ZnII, CdII), formed from 4-fold-symmetric ZnII-porphyrin-centered tetrakis-meso-(5¤-methyl-2,2¤-bipyridyl) ligands. The structures of these two D3-symmetric cages have been characterized by 1D and 2D NMR, ESI-MS, and XRD analyses. A common structural feature of these complexes is their inner molecular binding site at the axial position of each square-pyramidal ZnII-porphyrin in the crystal structure, which would provide a method to place molecular coordination sites inside or outside the cage complex with the minimum chemical modification.
- Iizuka, Fumiya,Nakamura, Takashi,Sato, Hiroyasu,Shionoya, Mitsuhiko,Ube, Hitoshi
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Read Online
- Preparation method of 2-bromo-5-aldehyde pyridine
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The invention relates to a preparation method of 2-bromo-5-aldehyde pyridine, and the method comprises the following steps: 1) dissolving 2, 5-dibromo pyridine in a solvent A, adding a Grignard reagent, and carrying out a Grignard exchange reaction; 2) adding DMF until the reaction is finished to obtain the 2-bromo-5-aldehyde pyridine. The preparation method disclosed by the invention is simple and mild in process conditions and low in preparation cost, and the prepared target product is high in yield and purity and suitable for industrial large-scale production.
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Paragraph 0025; 0031-0038
(2021/03/13)
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- NOVEL COMPOUNDS FOR INHIBITION OF JANUS KINASE 1
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An object of the invention is to provide compounds as selective JAK1 inhibitor, a process for preparation of the inhibitors, a composition containing the compounds and utility of the compounds.
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Page/Page column 100; 117
(2020/12/11)
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- A Transition-Metal-Free One-Pot Cascade Process for Transformation of Primary Alcohols (RCH2OH) to Nitriles (RCN) Mediated by SO2F2
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A new transition-metal-free one-pot cascade process for the direct conversion of alcohols to nitriles was developed without introducing an “additional carbon atom”. This protocol allows transformations of readily available, inexpensive, and abundant alcohols to highly valuable nitriles.
- Jiang, Ying,Sun, Bing,Fang, Wan-Yin,Qin, Hua-Li
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supporting information
p. 3190 - 3194
(2019/05/21)
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- Preparation method of 2-bromine-5-formylpyridine
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The invention relates to the field of fine chemical industry and particularly relates to a preparation method of 2-bromine-5-formylpyridine. The preparation method comprises the following steps: (1) performing an oxidation reaction; (2) performing a bromination reaction. In the preparation method provided by the invention, 2-chlorine-5-chloromethyl pyridine is taken as a raw material, and the 2-bromine-5-formylpyridine is prepared by two steps of reactions: the oxidation reaction and the bromination reaction, so that the method is simple in technological operation, mild and safe in reaction conditions, low in cost of the raw material, high in reaction conversion rate, high in yield and easy in extraction of a product, therefore, the method is more suitable for safe industrial production and has greater implementation value and social and economic benefits.
- -
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Paragraph 0086; 0087; 0088; 0089
(2018/04/02)
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- PISTON FOR AN INTERNAL COMBUSTION ENGINE AND METHOD FOR PRODUCING THE PISTON FOR AN INTERNAL COMBUSTION ENGINE
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The present invention relates to compounds of general formula (I), wherein A represents an optionally substituted heterocycle group, B represents an aryl or heteroaryl group and wherein X, R1, R2, R3, R4 and R5 are as defined in the description. Compounds of formula (I) are useful to destroy, inhibit, or prevent the growth or spread of cells, especially malignant cells, into surrounding tissues implicated in a variety of human and animal diseases.
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- 2-bromo-5-formyl-pyridine preparation method
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The invention relates to the field of fine chemical engineering, in particular to a 2-bromo-5-formyl-pyridine preparation method. The method includes steps: 1) subjecting 2-chloro-5-chloromethylpyridine to bromination reaction in presence of a bromination reagent to obtain 2-bromo-5-bromomethylpyridine; 2) subjecting 2-bromo-5-bromomethylpyridine to oxidation reaction under action of an oxidation reagent and alkali metal salt to obtain 2-bromo-5-formyl-pyridine. According to the preparation method, 2-bromo-5-formyl-pyridine is prepared from 2-chloro-5-chloromethylpyridine through a two-step reaction of bromination and oxidation, technical simplicity in operation, safe and mild reaction conditions, low raw material cost, high reaction conversion rate, high yield and easiness in product extraction are realized. Therefore, the method is suitable for industrial safety production and high in implementation value and social economical benefits.
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Paragraph 0078; 0081; 0084; 0087; 0090
(2017/10/28)
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- Spin-dimer networks: Engineering tools to adjust the magnetic interactions in biradicals
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Magneto-structural correlations in stable organic biradicals have been studied on the example of weakly exchange coupled models with nitronyl nitroxide and imino nitroxide spin-carrying entities. Here, heteroatom substituted 2,2′-diaza- and 3,3′-diaza-tolane bridged biradicals were compared with the hydrocarbon analogue, while a biphenyl model with its 2,2′-bipyridine counterpart. For a 3,3′-diazatolane bridge the torsional angle between the nitronyl nitroxides and the pyridyl rings increased heavily (~52-54°) leading to a smaller theoretical intra-dimer exchange coupling value. However, a very large antiferromagnetic coupling was obtained experimentally. This could be appropriately explained by the presence of dominating inter-dimer exchange between the molecules. For the bis(imino nitroxide) with tolane bridge a field induced ordered state between 1.8 to 4.3 T in AC-susceptibility measurements was observed. In terms of a Bose Einstein condensate (BEC) of triplons this phenomenon could be described as a magnetic field induced ordered phase with 3D character.
- Borozdina, Yulia B.,Mostovich, Evgeny A.,Cong, Pham Thanh,Postulka, Lars,Wolf, Bernd,Lang, Michael,Baumgarten, Martin
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p. 9053 - 9065
(2017/09/22)
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- Pyrimidine derivative substitued with pyridyl group, and organic electroluminescent device including the same
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The present invention provides a pyrimidine derivative having a pyridyl group bonded thereto represented by chemical formula 1 in figure 1. In the chemical formula 1, Ar_1 and Ar_2 are each independently C6-C30 aryl or C5-C30 heteroaryl; X_1 and X_2 are each independently CH or N (provided that one of X_1 and X_2 is N); and R_1 is selected from the group consisting of hydrogen, halogen, amino, nitro, cyano, hydroxy, a diphenylphosphino group, a diphenyl phosphooxide group, C1-C10 alkyl, C3-C8 cycloalkyl, C6-C30 silyl, C1-C20 alkoxy, C6-C20 aryloxy, C1-C20 alkylthio, C6-C30 aryl, C6-C30 aralkyl, C1-C10 heteroalkyl, C2-C8 heterocycloalkyl, C5-C30 heteroaryl, C5-C30 heteroaralkyl, or C6 -C20 arylthio. When the pyrimidine derivative having the pyridyl group bonded thereto is used as an element for forming an organic material layer of an organic electronic device, the efficiency of the device and the stability of the element can be enhanced and the driving voltage can be dropped.COPYRIGHT KIPO 2017
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Paragraph 0083-0086
(2017/09/14)
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- Pyrimidine derivatives substituted with heteroaryl substituted-pyridyl or -phenyl, and organic electroluminescent device including the same
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Provided are pyrimidine derivatives represented by chemical formula 1 and bonded with a heteroaryl substituted-pyridyl or -phenyl group. In the chemical formula 1, Ar_1 and Ar_2 are each independently an aryl having 6-30 carbon atoms, or a heteroaryl having 5-30 carbon atoms; X_1 and X_2 are each independently CH or N, but are not simultaneously N; A is a phenyl group, a pyridyl group, or a naphthyl group; and B has a structure represented by chemical formula 2.COPYRIGHT KIPO 2017
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Paragraph 0096-0099
(2017/09/29)
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- Pyrimidine derivative substitued with pyridyl group, and organic electroluminescent device including the same
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Provided is a pyrimidine derivative bonded with a pyridyl group represented by chemical formula 1. In the chemical formula 1: Ar_1 and Ar_2 are each independently an aryl having 6-30 carbon atoms, or a heteroaryl having 5-30 carbon atoms; X_1 and X_2 are each independently CH or N, while at least one of X_1 and X_2 is N; and A has a structure represented by chemical formula 2.COPYRIGHT KIPO 2017
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Paragraph 0078-0081
(2017/10/20)
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- METALLOENZYME INHIBITOR COMPOUNDS
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The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
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Page/Page column 165; 166
(2017/07/31)
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- Metal complex containing carbazoles connected Phenyl-pyridine, it's preparation method and it's applications
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PURPOSE: A phenyl-pyridine metal complex compound which is connected with carbazole structure is provided to enhance high electroluminescence(EL) intensity at 700-750 nm. CONSTITUTION: A metal complex compound contains a phenylpyridine structure which is connected with carbazole structure of chemical formula 1. In chemical formula 1, M is metal having an atom weight of 40 or more; X-Y is auxiliary ligand; R1 is alkyl of 1-16 carbon atoms or alkyl ether group of 1-16 carbon atoms; and R2 and R3 are F or CF_3 each. A light emitting device contains the metal complex compound. A sensor is manufactured using the light emitting device.
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Paragraph 0022-0023
(2017/04/03)
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- COMPOUNDS WITH ANTI-TUMORAL ACTIVITY
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The present invention relates to compounds of general formula (I), wherein A represents an optionally substituted heterocycle group, B represents an aryl or heteroaryl group and wherein X, R1, R2, R3, R4 and R5 are as defined in the description. Compounds of formula (I) are useful to destroy, inhibit, or prevent the growth or spread of cells, especially malignant cells, into surrounding tissues implicated in a variety of human and animal diseases.
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- Formylated chloro-bridged iridium(iii) dimers as OLED materials: Opening up new possibilities
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In this study, a series of four formyl-substituted chloro-bridged iridium(iii) dimers were prepared. Their absorption, photophysical and electrochemical properties were studied in dichloromethane solution. It was found that as the formyl content increased on the cyclometalating ligands, emission unexpectedly became brighter. Organic light-emitting diodes (OLEDs) were fabricated using each of these iridium dimers as the emitter. The OLED fabricated using the brightest of the series, 2b, as the dopant afforded a decent external quantum efficiency (EQE) of 2.6%. This suggests that chloro-bridged iridium dimers are potential candidates as solid-state emitters. This journal is
- Wong, Michael Y.,Xie, Guohua,Tourbillon, Clarisse,Sandroni, Martina,Cordes, David B.,Slawin, Alexandra M. Z.,Samuel, Ifor D.W.,Zysman-Colman, Eli
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p. 8419 - 8432
(2015/05/13)
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- Lewis basicity modulation of N-heterocycles: A key for successful cross-metathesis
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Cross-metathesis involving N-heteroaromatic olefinic derivatives is disclosed. The introduction of an appropriate substituent on the heteroaromatic ring decreases the Lewis basicity of the nitrogen atom, thus preventing the deactivation of the ruthenium-centered catalyst. The reaction is quite general in terms of both N-heterocycles and olefinic partners.
- Lafaye, Kevin,Nicolas, Lionel,Gurinot, Amandine,Reymond, Sbastien,Cossy, Janine
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supporting information
p. 4972 - 4975
(2015/01/08)
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- Cushing's syndrome: Development of highly potent and selective CYP11B1 inhibitors of the (pyridylmethyl)pyridine type
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Potent and selective CYP11B1 inhibitors could be promising therapeutics for the treatment of Cushing's syndrome. Optimization of Ref 1 (5-((1H-imidazol-1- yl)methyl)-2-phenylpyridine) led to compound 44 (5-((5-methylpyridin-3-yl) methyl)-2-phenylpyridine) with a 50-fold improved IC50 value of 2 nM toward human CYP11B1 and an enhanced inhibition of the rat enzyme (IC 50 = 2440 nM) compared to Ref 1 (IC50 > 10000 nM). Furthermore, selectivities over CYP11B2, CYP17, and CYP19 were observed, as well as satisfying metabolic stability not only in human and rat plasma but also in liver S9 fraction. Investigation of cytotoxicity and inhibition of hepatic CYP2A6 and CYP3A4 showed that 44 fulfills first safety criteria and can be considered for further in vivo evaluation in rats.
- Emmerich, Juliette,Hu, Qingzhong,Hanke, Nina,Hartmann, Rolf W.
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p. 6022 - 6032
(2013/09/02)
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- New ternary ligands consisting of an N4 bridging ligand and two terpyridines, and their Co(ii) and Ni(ii) dinuclear complexes. Structure, redox properties, and reaction with acid
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Two ternary ligands consisting of two 2,2′:6′,2′′- terpyridines and one N4-quadridentate μ2,η2- bridging ligand were synthesized. The N4 bridge is 1,4-bis(2-pyridyl)phthalazine in ligand 1, and 3,6-bis(2-pyridyl)pyridazine in ligand 2. Two Co(ii) dinuclear complexes [(1)Co2(μ-OH)]3+ and [(2)Co 2(μ-OH)]3+, and one Ni(ii) dinuclear complex [(1)Ni2(μ-Cl)]3+ were obtained. In the crystal structures of [(1)Co2(μ-OH)]3+ and [(1)Ni 2(μ-Cl)]3+, two pyridine rings are twisted around the pyridine-phthalazine bonds to avoid steric repulsion between the hydrogen atoms. The pyridine rings also showed a significant tilt from the octahedral coordination plane, which causes the large positive shift of the first reduction potentials. Upon the addition of a proton, the cobalt dinuclear complexes can release one cobalt ion selectively, and the dinuclear complexes can be easily restored by the addition of a tertiary amine.
- Kon, Hiroki,Nagata, Toshi
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p. 5697 - 5705
(2013/07/05)
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- SELECTIVE CYP11B1 INHIBITORS FOR THE TREATMENT OF CORTISOL DEPENDENT DISEASES
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The present invention relates to compounds which selectively inhibit CYP11B1. Preferably, the compounds of the present invention do not substantially inhibit CYP11B2. Moreover, the compounds of the present invention do not substantially inhibit CYP17 and/or CYP19, either. Amongst other applications of the compounds of the present invention, they can be used for the treatment of Cushing's syndrome or metabolic disease.
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Page/Page column 59
(2012/05/05)
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- METALLOENZYME INHIBITOR COMPOUNDS
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The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
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Page/Page column 68-72
(2013/02/28)
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- A METHOD OF TREATING LIVER FIBROSIS
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The present invention relates to a method of treating hepatis C and/or liver fibroisis with 3-cycloalkylaminopyrrolidine derivatives of the present invention
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Page/Page column 42
(2012/09/11)
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- UREA INHIBITORS OF MAP KINASES
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Urea containing compounds that inhibit MAP kinases, pharmaceutical compositions including such compounds and methods for using these compounds to treat inflammatory diseases and cancer are described herein.
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Page/Page column 26-27
(2010/03/04)
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- BIARYLRHODANINE AND PYRIDYLRHODANINE COMPOUNDS AND THEIR USE
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The present invention pertains generally to the field of therapeutic compounds, and more specifically to compounds related to rhodanine, which compounds are inter alia inhibitors and/or binders of antiapoptotic/pro-survival Bcl-2 proteins such as Bcl-XL and/or Mcl-1. More specifically, the present invention is concerned with Rhodanine- based Pan-Bcl-2 inhibitors and Mcl-1 -specific inhibitors as anti-cancer compounds. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and invivo, to inhibit and/or bind Bcl-2 proteins such as Bcl-XL and/or Mcl-1, and in the treatment of diseases and conditions that are mediated by Bcl-2 proteins, that are ameliorated by the inhibition of Bcl-2 protein function (such as Bcl-XL and/or Mcl-1 ) including proliferative conditions such as cancer, optionally in combination with another agent.
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Page/Page column 81; 82
(2010/04/06)
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- Structural insights into the design of small molecule inhibitors that selectively antagonize Mcl-1
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The screening of a small focused library of rhodanine derivatives as inhibitors of Bcl-2 proteins led to the discovery of two structurally related compounds with different binding profiles against the Bcl-XL and the Mcl-1 proteins. Subsequent NMR studies with mutant proteins and in silico docking studies provide a possible rationale for the observed specificity.
- Bernardo, Paul H.,Sivaraman, Thirunavukkarasu,Wan, Kah-Fei,Xu, Jin,Krishnamoorthy, Janarthanan,Sons, Chun Meng,Tian, Liming,Chin, Jasmine S. F.,Lim, Diane S. W.,Mok, Henry Y. K.,Yu, Victor C.,Tong, Joo Chuan,Chai, Christina L. L.
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supporting information; experimental part
p. 2314 - 2318
(2010/08/06)
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- Heteroaryl-substituted amides comprising an unsaturated or cyclic linker group, and their use as pharmaceuticals
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The present invention relates to N-alkylamides of the formula I, in which A, Het, X, R 1 , R 2 and R 3 have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of the formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired. The invention further relates to processes for the preparation of compounds of the formula I, to pharmaceutical compositions comprising them, and to the use of compounds of the formula I for the manufacture of a medicament for the stimulation of the expression of endothelial NO synthase or for the treatment of various diseases including cardiovascular disorders such as atherosclerosis, thrombosis, coronary artery disease, hypertension and cardiac insufficiency, for example.
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Page/Page column 47
(2008/06/13)
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- DISUBSTITUTED THIENYL COMPOUNDS AND THEIR USE AS PHARMACEUTICALS
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The present invention relates to modulators of HM74a receptor, and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with HM74a receptor.
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Page/Page column 55-56
(2010/11/25)
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- 3-Cycloalkylaminopyrrolidine derivatives as modulators of chemokine receptors
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The present invention relates to 3-cycloalkylaminopyrrolidine derivatives of the formula I: (wherein R1, R2, R3, R4, R5, R6, R7, X, Y and Z are as defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of chemokine receptors and more specifically as modulators of the CCR2 and/or CCR5 receptor. The compounds and compositions of the invention may bind to chemokine receptors, e.g., the CCR2 and/or CCR5 chemokine receptors, and are useful for treating diseases associated with chemokine, e.g., CCR2 and/or CCR5, activity, such as atherosclerosis, restenosis, lupus, organ transplant rejection and rheumatoid arthritis.
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Page/Page column 24
(2008/06/13)
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- The expedient access to bromo-pyridine carbaldehyde scaffolds using gem-dibromomethyl intermediates
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A simple, efficient, and general two-step synthesis to bromo-pyridine carbaldehyde scaffolds is described. This direct route involves sequential reactions employing the dibromination of bromo-picolines followed by hydrolysis using an aqueous solution of calcium carbonate. Bromo-pyridine carbaldehyde scaffolds 1-7 were obtained in good overall yield. Bromo-dibromomethyl-pyridine intermediates have been isolated and characterized.
- Mandal, Ashis Baran,Augustine, John Kallikat,Quattropani, Anna,Bombrun, Agnes
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p. 6033 - 6036
(2007/10/03)
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- SELECTIVE ESTROGEN RECEPTOR MODULATORS
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The present invention provides a compound represented by the following formula (I); [wherein T represents a single bond, a C1-C4 alkylene group which may have a substituent and the like; formula (I-1) represents a single bond or a double bond; A represents a single bond, a bivalent 5- to 14-membered heterocyclic group which may have a substituent and the like; Y represents a single bond and the like; Z represents a methylene group and the like; ring G represents a phenylene group and the like which may condense with a 5- to 6-membered ring and may have a heteroatom; Ra and Rb are the same as or different from each other and represent a hydrogen atom and the like; W represents a single bond and the like; R' represents 1 to 4 independent hydrogen atoms and the like; and R" represents 1 to 4 independent hydrogen atoms and the like] or a salt thereof, or a hydrate thereof.
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Page/Page column 104
(2008/06/13)
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- MUSCARINIC ANTAGONISTS
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Heterocyclic derivatives of di-N-substituted piperazine or 1,4 di-substituted piperidine compounds in accordance with formula (I) (including all isomers, salts and solvates), wherein one of Y and Z is -N- and the other is -N- or -CH-; X is -O-, -S-, -SO-, -SO2- or -CH2-; Q is (1), (2), (3); R is alkyl, cycloalkyl, optionally substituted aryl or heteroaryl; R, R and R are H or alkyl; R is alkyl, cyclolalkyl or (4); R is H, alkyl, -C(O)alkyl, arylcarbonyl, -SO2alkyl, aryl-sulfonyl-C(O)Oalkyl, aryloxycarbonyl, -C(O)NH-alkyl or aryl-aminocarbonyl, wherein the aryl portion is optionally substituted; R is H or alkyl; and R is H, alkyl, hydroxyalkyl or alkoxyalkyl; are muscarinic antagonists useful for treating cognitive disorders such as Alzheimer's disease. Pharmaceutical compositions and methods of treatment are also disclosed.
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- Synthesis of a Non-Heme Template for Attaching Four Peptides: An Approach to Artificial Iron (II)-Containing Peroxidases
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We are developing all-synthetic model cofactor-protein complexes in order to define the parameters controlling non-natural cofactor activity. The long-term objective is to establish the theoretical and practical basis for designing novel enzymes. A non-heme pentadentate ligand (N4Py) is being developed as a template for the site-specific attachment of a designed four-helix bundle. Previously, we attached two unprotected peptides via CH 2Cl handles to N4Py. In the presence of hydrogen peroxide, the iron(II) complex of this ligand (2a) generates an FeIIIOOH intermediate (3a) that can oxidize a wide variety of organic compounds. Here, we describe the synthesis of 27, a N4Py derivative in which four three-carbon spacers have been introduced, and show that four copies of an unprotected, single-cysteine peptide can be coupled via a thioether linkage to the ligand. In addition, a divergent synthesis route to tetrabromide ligand lb has also been developed, providing the opportunity to prepare alternative pentadentate ligands efficiently by four cross-coupling reactions on a single molecule. Also, two of the four bromides of lb can be selectively addressed by magnesium-bromide exchange.
- Van Den Heuvel, Marco,Van Den Berg, Tieme A.,Kellogg, Richard M.,Choma, Christin T.,Feringa, Ben L.
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p. 250 - 262
(2007/10/03)
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- A multifunctional high-spin biradical pyrazolylbipyridine- bisnitronylnitroxide
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(Chemical Equation Presented) Synthesis and UV-vis, IR, and EPR spectroscopic characterizations, together with X-ray structural analysis, of functional nitronyl- and iminonitroxides attached to pyrazolylbipyridine are described. The exchange interactions between the nitronylnitroxides are found to be stronger than for the iminonitroxides. Although the substitution of a pyridine with the pyrazole ring leads to shorter distances and larger dipolar couplings, the exchange interaction is diminished. While compound 1 forms dimers in the solid state, the terpyridine 3 leads to supramolecular π-stacking.
- Zoppellaro, Giorgio,Enkelmann, Volker,Geies, Ahmed,Baumgarten, Martin
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p. 4929 - 4932
(2007/10/03)
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- Oxime derivatives for the treatment of dyslipidemia and hypercholesteremia
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The present invention relates to compounds of Formula (I) which may be useful in the treatment of diseases, such as, metabolic disorders, dyslipidemia and/or hyperchloesterolemia: 1
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- Method of converting functional group through halogen-metal exchange reaction
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A method by which a halogen atom of a halogen compound can be efficiently replaced with an electrophilic group. Also provided are: a reagent for converting a functional group through a halogen-metal exchange reaction, characterized by comprising either a mixture of a magnesium compound represented by the formula R1—Mg—X (I) (wherein R1 represents a halogen atom or an optionally substituted hydrocarbon residue; and X1 represents a halogen atom) and an organolithium compound represented by the formula R2—Li (II) (wherein R2 represents an optionally substituted hydrocarbon residue) or a product of the reaction of the magnesium compound with the organolithium compound; and a process for producing with the reagent a compound in which a halogen atom of a halogen compound has been replaced with an electrophilic group.
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- Synthesis of a Hexagonal Nanosized Macrocyclic Fluorophore with Integrated Endotopic Terpyridine Metal-Chelation Sites
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A rigid nanosized hexagonal phenylethynyl cyclophane 5 has been prepared, which incorporates two 2,2′:6′,2″-terpyridines as integral structural units, for the purpose of binding metal ions. Macrocycle 5 was obtained by a 14-step synthesis in an overall yield of 11%, and was characterised by spectroscopic techniques. The efficiency and ease of all transformations, and the relatively enhanced yield of the final macrocyclisation suggests that the entire synthetic pathway should be amenable to scale-up. Cyclophane 5 possesses four bulky triisopropylsilyl(TIPS) -protected ethyne substituents which serve a dual role. Firstly, they solubilise the structure thereby facilitating purification and subsequent handling. Secondly, they enable post-synthetic modification in which additional functionality may be attached to the periphery of the ring. Significantly, 5 was found to be a fluorescent chromophore, and may therefore potentially function as a new sensory platform for the detection of metal ions and H-bond donating biological substrates. The structurally well-defined nanosized morphology of 5, coupled with its interesting spectroscopic properties, supports the expectation that 5 and related architectures will attain a wealth of future applications within the developing fields of nanochemistry and nanoscience.
- Baxter, Paul N. W.
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p. 5011 - 5022
(2007/10/03)
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- Telomerase inhibitors and methods of their use
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Thiazolidinedione compounds, compositions, and methods of inhibiting telomerase activity in vitro and treatment of telomerase mediated conditions or diseases ex vivo and in vivo are provided. The methods, compounds and compositions of the invention may be employed alone, or in combination with other pharmacologically active agents in the treatment of conditions or diseases mediated by telomerase activity, such as in the treatment of cancer. Also disclosed are methods for assaying or screening for inhibitors of telomerase activity.
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- Tributylmagnesium ate complex-mediated novel bromine-magnesium exchange reaction for selective monosubstitution of dibromoarenes
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Lithium tributylmagnesate complex (n-Bu3MgLi), readily prepared from n-BuLi and n-BuMgCl (2:1), is a novel metallation agent. It is quite efficient for the selective mono-bromine-magnesium exchange of 2,6-dibromopyridine (1) under non-cryogenic conditions (at -10°C) to give a stable magnesate intermediate. Subsequent treatment with DMF gave 6-bromo-2-formylpyridine (3) in excellent yield. This method is also applicable for selective monosubstitution of several other kinds of dibromoarenes.
- Iida, Takehiko,Wada, Toshihiro,Tomimoto, Koji,Mase, Toshiaki
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p. 4841 - 4844
(2007/10/03)
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- Formylations of anions with a 'Weinreb' formamide: N-methoxy-N-methylformamide
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Treatment of organolithiums, Grignard reagents, or enolates with N-methoxy-N-methylformamide leads to formylated products in good yields without competing secondary processes.
- Lipshutz, Bruce H.,Pfeiffer, Steven S.,Chrisman, Will
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p. 7889 - 7892
(2007/10/03)
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- Substituted dipyridylethenes and -ethynes and key pyridine building blocks
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Various new 2,5-disubstituted pyridines were prepared. The 2-substituted 5-formylpyridines 8, 15a-b were obtained by reduction of the nicotinic acid 3, hydrolysis of the bis(morpholino)methylpyridine 6 or the reaction of 5-bromopyridines 12 and 14 with lithium butoxide in DMF. Dipyridylethenes 16a-b,e were synthesized by Wadsworth-Emmons reaction with pyridyl phosphonate 7 or by coupling of the aldehydes by McMurry reaction to the ethenes 16c-d. After bromination of the C = C double bond of the dipyridylethenes 16a-d, dipyridylacetylenes 18a-d were obtained via elimination of the 1,2-dipyridyl-1,2-dibromoethanes 17a-d.
- Windscheif,Vogtle
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