- Alkylation and arylation of pyrazoles under solvent-free conditions: Conventional heating versus microwave irradiation
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The use of sodium hydrogen carbonate under solvent-free conditions and microwave irradiation is by far the best method for N-alkylating pyrazoles. The yields are good and the method is devoid of side reactions (quaternization, isomerization, hydrogen hali
- Almena, Ines,Diez-Barra, Enrique,De La Hoz, Antonio,Ruiz, Juliana,Sanchez-Migallon, Ana,Elguero, Jose
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- Molecular tectonics: Dimensionality and geometry control of silver coordination networks based on pyrazolyl appended thiacalixarenes
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Combinations of six new coordinating tectons (3-8) tetrakis-pyrazolyl appended calix[4]arenes, blocked in 1,3-A conformation, based on 1 (tetrathiacalix[4]arene) and 2 (tetrathiatetramercaptocalix[4]arene) derivatives, with AgX salts (X = NO3-, BF4-, XF6- (X = P, As and Sb)) lead to nine new silver coordination networks. The flexible nature of tectons 3-8 (length of the spacer between the macrocycle and the pyrazolyl coordinating unit), their high number of potential coordinating sites and the loose coordination demand of Ag+ cation lead to the formation of a large variety of networks with different dimensionality: from 1D (5-AgSbF6, 5-AgBF4, 7-AgSbF6 and 8-AgNO3) to extended 2D (6-AgBF4 and 8-AgSbF6) and to a series of three isostructural porous diamond-like 3D architectures (6-AgXF6 (X = P, As and Sb)).
- Ovsyannikov,Noamane,Abidi,Ferlay,Solovieva,Antipin,Konovalov,Kyritsakas,Hosseini
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p. 691 - 703
(2016/07/12)
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- HYDROXAMATE-BASED INHIBITORS OF DEACETYLASES B
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The present teachings relate to compounds of Formula I: and pharmaceutically acceptable salts, hydrates, esters, and prodrugs thereof, wherein R1, R2, R3, Y, Z, and are as defined herein. The present teachings also provide methods of preparing compounds of Formula I and methods of using compounds of Formula I in treating, inhibiting, or preventing pathologic conditions or disorders mediated wholly or in part by deacetylases.
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Page/Page column 40
(2009/10/06)
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- Preparation of annulated nitrogen-containing heterocycles via a one-pot palladium-catalyzed alkylation/direct arylation sequence
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A palladium-catalyzed/norbornene-mediated sequential coupling reaction involving an aromatic sp2 C-H functionalization as the key step is described, in which an alkyl-aryl bond and an aryl-heteroaryl bond are formed in one pot. A variety of hig
- Blaszykowski, Christophe,Aktoudianakis, Evangelos,Bressy, Cyril,Alberico, Dino,Lautens, Mark
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p. 2043 - 2045
(2007/10/03)
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- Rhodium(I) and iridium(I) complexes with bidentate N,N and P,N ligands as catalysts for the hydrothiolation of alkynes
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Cationic iridium(I), rhodium(I) complexes containing bis(1-methylimidazol-2-yl)methane, bim, [M(bim)(CO)2]BPh4 (M = Ir (1), Rh (2)); bis(pyrazol-1-yl)methane, bpm, [M(bpm)(CO)2]BPh4 (M = Ir (3), Rh (4)) have bee
- Burling, Suzanne,Field, Leslie D.,Messerle, Barbara A.,Vuong, Khuong Q.,Turner, Peter
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p. 4181 - 4191
(2007/10/03)
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- N-2-(Azol-1(2)-yl)ethyliminodiacetic acids: A novel series of Gd(III) chelators as T2 relaxation agents for magnetic resonance imaging
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The synthesis, physicochemical properties, and toxicological implications of a novel series of N-2-(azol-1(2)-yl)ethyliminodiacetic acids, useful as contrast agents for magnetic resonance imaging are reported. Compounds were prepared by alkylation of methyl iminodiacetate with N-2-bromoethylazoles and subsequent hydrolysis. Stability constants of the corresponding Gd(III) complexes and T1 and T2 relaxivities were determined and interpreted in terms of optimized geometries obtained by semiempirical PM3 calculations. Compounds show increased T2 relaxivity and decreased toxicity in vitro as compared to EDTA-Gd(III) complexes. Copyright (C) 1999 Elsevier Science Ltd.
- Lopez, Pilar,Seipelt, Christa G.,Merkling, Patrick,Sturz, Laszlo,Alvarez, Jose,Doelle, Andreas,Zeidler, Manfred D.,Cerdan, Sebastian,Ballesteros, Paloma
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p. 517 - 527
(2007/10/03)
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- Synthesis, structure (NMR and mass spectrometry) and conformational analysis of heterocyclic analogues of dibenzocycloocta-1,5-diene: 5,6,12,13-tetrahydrobispyrazotetraazocinediium dihalides
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Several 5,6,12,13-tetrahydrobispyrazotetraazocinediium dihalides 4a-d and 8 are prepared from pyrazole, 3,5-dimethylpyrazole, 4-(1-adamantyl)pyrazole and camphopyrazole by stepwise alkylation with 1,2-dibromoethane or 1,2-dichloroethane.Their structural characterization has been achieved by NMR and mass spectrometry.Dynamic NMR spectroscopy allowed the measurement of the barrier for the chair-chair interconversion in the case of the parent compound 4a and the 1,3,8,10-tetramethyl derivative 4b.These barriers as well as the preferred chair conformation are rationalized through semi-empirical and molecular mechanics calculations with regard to dibenzocycloocta-1,5-diene.The study of doubly charged bispyrazolium salts allows demonstration of their reduction by addition of a hydride ion ++ + H- -> (C + H)+> during FABMS experiments.
- Cabildo, Pilar,Claramunt, Rosa M.,Cornago, Pilar,Lavandera, Jose Luis,Sanz, Dionisia,et al.
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p. 701 - 712
(2007/10/03)
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- Cyclometallation of polydentate ligands containing pyrazole groups, including the synthesis of platinum(IV) complexes with tripodal - ligand systems
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Dimethylplatinum(II) complexes, PtR2(L), have been made by reaction of 2 with a range of polydentate nitrogen donor ligands containing one or more pyrazol-1-yl (pz) donor groups, including the new ligand bis(pyrazol-1-yl)(thien-2-yl)methane.The complexes give cis-PtMe2(py)2 when dissolved in pyridine at ambient temperature, except for PtMe2(L) (L = (pz)2CH2, (pz)2C(H)Ph, (pz)3CH, or (pz)2(mim)CH (mim = N-methylimidazol-2-yl)), which undergo cyclometallation at a C(5) position of one pyrazol-1-yl ring.The cyclometallated ligands have been examined as 'isoelectronic' analogues of nitrogen donor poly(pyrazol-1-yl)alkane and poly(pyrazol-1-yl)borate ligands.A carbon monoxide derivative, PtMe(CO) (1d) and a series of phosphine complexes have been prepared.The complex PtMe(py) (1a) and polymeric >n (2) undergo oxidative addition reactions with organohalides to give the platinum(IV) complexes (py)>X (7a-d) and fac-PtXMe(R) (8a-b), respectively.The new reagent 1-bromo-2-(pyrazol-1-yl)ethane forms (pzCH2CH2-N,C)>Br (10), containing both - and - ligands.Reaction of MeI or PhCH2Br with PtMe2> gives fac-PtXMe(R) (8a,b) directly, and PtMe2 undergoes a similar cyclometallation/oxidative addition in iodomethane to form fac-PtIMe2 (13).
- Canty, Allan J.,Honeyman, Thomas R.
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p. 247 - 263
(2007/10/02)
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