- Relayed Regioselective Alkynylation/Olefination of Unsymmetrical Cyclic Diaryliodonium Species Catalyzed by Cu and Pd: Affording Fluorescent Cytotoxic Benzoxazoles
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Although cyclic diaryliodonium species have the potential to act as valuable synthons for cascade transformations, they still remain largely unexplored. The regioselectivity associated with unsymmetrical cyclic diaryliodonium species has previously been k
- Zhu, Daqian,Liu, Panpan,Lu, Wenhua,Wang, Haiwen,Luo, Bingling,Hu, Yumin,Huang, Peng,Wen, Shijun
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Read Online
- Benzotriazine compound with PAR4 antagonistic activity and application thereof
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The invention discloses a benzotriazine compound with PAR4 antagonistic activity and application thereof. The present invention relates to a compound of formula (I) or a stereoisomer, tautomer, pharmaceutically acceptable salt, ester, solvate or prodrug t
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Paragraph 0059; 0061; 0066
(2020/08/02)
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- Effects of Thiolate Ligation in Monoiron Hydrogenase (Hmd): Stability of the {Fe(CO)2}2+ Core with NNS Ligands
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In this work, we report the effects of NNS-thiolate ligands and nuclearity (monomer, dimer) on the stability of iron complexes related to the active site of monoiron hydrogenase (Hmd). A thermally stable iron(II) dicarbonyl motif is the core feature of th
- Xie, Zhu-Lin,Pennington, Doran L.,Boucher, Dylan G.,Lo, James,Rose, Michael J.
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p. 10028 - 10039
(2018/08/28)
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- Design, synthesis and structure–activity relationships of novel phenylalanine-based amino acids as kainate receptors ligands
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A new series of carboxyaryl-substituted phenylalanines was designed, synthesized and pharmacologically characterized in vitro at native rat ionotropic glutamate receptors as well as at cloned homomeric kainate receptors GluK1–GluK3. Among them, six compounds bound to GluK1 receptor subtypes with reasonable affinity (Kivalues in the range of 4.9–7.5?μM). A structure–activity relationship (SAR) for the obtained series, focused mainly on the pharmacological effect of structural modifications in the 4- and 5-position of the phenylalanine ring, was established. To illustrate the results, molecular docking of the synthesized series to the X-ray structure of GluK1 ligand binding core was performed. The influence of individual substituents at the phenylalanine ring for both the affinity and selectivity at AMPA, GluK1 and GluK3 receptors was analyzed, giving directions for future studies.
- Szymańska, Ewa,Cha?upnik, Paulina,Szczepańska, Katarzyna,Cu?ado Moral, Ana Maria,Pickering, Darryl S.,Nielsen, Birgitte,Johansen, Tommy N.,Kie?-Kononowicz, Katarzyna
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supporting information
p. 5568 - 5572
(2016/11/09)
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- Synthesis of 6,6′-bis(dimethylamino)- and 6,6′-dibromo- substituted 2,2′-diphosphanylbiphenyls and their palladium complexes
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New 6,6′-dibromo- and 6,6′-bis(dimethylamino)-substituted 2,2′-diphosphanylbiphenyl ligands 11-14 were prepared starting from 2,2′-dibromo-4,4′-dimethyl-6,6′-dinitro-1,1′-biphenyl (4). Depending on the phosphane groups [diphenylphosphanyl (11, 13) or diis
- Petzold, Holm,Alrawashdeh, Albara I. S.,Heider, Silvio,Haufe, Linda,Rueffer, Tobias
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p. 4858 - 4866
(2013/09/24)
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- The discovery of long-acting saligenin β2 adrenergic receptor agonists incorporating a urea group
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A series of novel, potent and selective human β2 adrenoceptor agonists incorporating a urea moiety on the terminal right-hand side phenyl ring of (R)-salmeterol is presented. Urea 9j had long duration of action in vitro on guinea pig trachea, and also in vivo similar to that of salmeterol. It had lower oral absorption and bioavailability than salmeterol in both rat and dog. It had a turnover ratio similar to salmeterol, with no evidence for formation of any aniline metabolites in human liver microsomes and hepatocytes. However no crystalline salts suitable for inhaled delivery were identified.
- Procopiou, Panayiotis A.,Barrett, Victoria J.,Ford, Alison J.,Looker, Brian E.,Lunniss, Gillian E.,Needham, Deborah,Smith, Claire E.,Somers, Graham
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experimental part
p. 6026 - 6032
(2011/11/07)
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- Synthesis of 4,4′-bisaryl-2,2′-bisbenzimidazoles as building blocks for supramolecular structures
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(Chemical Equation Presented) A series of 4,4′-bisaryl-2,2′- bisbenzimidazoles has been synthesized from the corresponding 4,4′-dibromo-2,2′-bisbenzimidazoles by Negishi coupling reactions. This procedure affords highly substituted bisbenzimidazoles.
- Yasui, Yoshizumi,Frantz, Derik K.,Siegel, Jay S.
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p. 4989 - 4992
(2007/10/03)
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- PHENETHANOLAMINE DERIVATIVES FOR TREATMENT OF RESPIRATORY DISEASES
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The present invention relates to novel compounds of formula (I),to a process for their manufacture, to pharmaceutical compositions containing them, and to their use in therapy, in particular their use in the prophylaxis and treatment of respiratory diseases.
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Page/Page column 78
(2010/02/07)
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- Benzo[1,2-c]1,2,5-oxadiazole N-Oxide Derivatives as Potential Antitrypanosomal Drugs. Structure-Activity Relationships. Part II
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The preparation of new derivatives of benzo[1,2-c]1,2,5-oxadiazole N-oxide is described. These derivatives were chosen in order to investigate and confirm previous structural features found necessary to display an adequate antitrypanosomal activity. The c
- Aguirre, Gabriela,Cerecetto, Hugo,Maio, Rossanna Di,Gonzalez, Mercedes,Porcal, Williams,Seoane, Gustavo,Ortega, Miguel A.,Aldana, Ignacio,Monge, Antonio,Denicola, Ana
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- Oxidative Bromination of Aromatic Amides using Sodium Perborate as Oxidant
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Sodium perborate in glacial acetic acid-acetic anhydride with potassium bromide and sodium tungstate as a catalyst, provides a novel system for the bromination of aromatic amides.
- Hanson, James R.,Harpel, Simone,Medina, Inmaculada C. Rodriguez,Rose, Dorian
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p. 432 - 433
(2007/10/03)
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- Herbicidal benzodioxoles and benzodioxanes
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Compounds of Formula I, and their N-oxides and agriculturally-suitable salts, are disclosed which are useful for controlling undesired vegetation STR1 wherein: STR2 T is O or S; W is a single bond, O, S or NR6 ; X is N or CH; Y is N or CH; Z is
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- Deuteriodediazoniation: A general method for the replacement of a diazonium group by deuterium
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Aromatic amino groups are replaced with deuterium via a diazonium salt intermediate. Dimethylformamide-d7 is the deuterium donor in this mild replacement method that yields aromatic-d1 products in high isotopic purity. The presence of methyl groups lowers the isotopic purity of the products.
- Wassmundt,Kiesman
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p. 281 - 288
(2007/10/02)
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- Catalysts for the Oxidative Bromination of Aromatic Amines and their N-Acetyl Derivatives
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In the nuclear bromination of aromatic amines by bromide and hydrogen peroxide in acetic acid, sodium tungstate has been compared with ammonium molybdate and ammonium vanadate, and found to be an effective catalyst.
- Hanson, James R.,Opakunle, Alexander,Petit, Philippe
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- Directed biosynthesis of 5'-fluoropactamycin in Streptomyces pactum
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A new pactamycin analogue, 5'-fluoropactamycin, was prepared by directed biosynthesis. Supplementation of the fermentation medium of Streptomyces pactum, var. pactum with 3-amino-5-fluorobenzoic acid, an analogue of 3-aminobenzoic acid, an advanced precursor in pactamycin biosynthesis, resulted in co-production of pactamycin and the new pactamycin analogue. A similar feeding experiment with 3-amino-5-methylbenzoic acid did not result in formation of the corresponding methylated pactamycin analogue, but only in inhibition of pactamycin production. Comparison of antimicrobial and cytotoxic activities of pactamycin and 5'-fluoropactamycin showed no significant differences.
- Adams,Rinehart
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p. 1456 - 1465
(2007/10/02)
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- Halogenation Using Quaternary Ammonium Polyhalides. VI. Bromination of Aromatic Amines by Use of Benzyltrimethylammonium Tribromide
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The reaction of aromatic amines with benzyltrimethylammonium tribromide in dichloromethane-methanol containing calcium carbonate powder for 0.5 h at room temperature gave bromo-substituted aromatic amines in good yields.
- Kajigaeshi, Shoji,Kakinami, Takaaki,Inoue, Kazuhisa,Kondo, Manabu,Nakamura, Hiroko,et al.
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p. 597 - 599
(2007/10/02)
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- Axially Dissymmetric Bis(triaryl)phosphines in the Biphenyl Series: Synthesis of (6,6'-Dimethylbiphenyl-2,2'-diyl)bis(diphenylphosphine) ('BIPHEMP') and Analogues, and their Use in Rh(I)-Catalyzed Asymmetric Isomerisations of N,N-Diethylnerylamine
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The axially dissymmetric diphosphines (-)-(R)- and (+)-(S)-(6,6'-dimethylbiphenyl-2,2'-diyl)bis(diphenylphosphine)((-)-(R)-10 and (+)-(S)-10; 'BIPHEMP') have been synthesized, starting from (R)- and (S)-6,6'-dimethylbiphenyl-2,2'-diamine ((R)- and (S)-16), respectively, via Sandmeyer reaction, lithiation, and phosphinylation.Moreover, racemic 4,4'-dimethyl- and 4,4'-bis(dimethylamino)-substituted analogues 11 and 12, respsctively, and the 6,6'-bridged analogue 1,11-bis(diphenylphosphino)-5,7-dihydrodibenzoxepin (13) were synthesized and resolved into optically pure (R)- and (S)-enantiomers via complexation with di-μ-chlorobisphenyl-C,N>dipalladium(II) ((R)-18).The molecular structures of the diphosphines (S)-10 and (R)-13 and of two derived cationic Rh(I) complexes, BF4 and BF4 were determined by X-ray analyses.Absolute configurations were established for (+)-(S)-10 by X-ray analyses of both the free diphosphine and of the derived Rh(I) complex, and for (-)-13 by X-ray analysis of the derived Rh(I) complex.Configurational assignments for the substituted BIPHEMP analogues 11 and 12 were achieved by means of 1H-NMR comparisons of the Pd(II) complexes derived from the diphosphines and (R)-18, and by means of CD comparisons.The BIPHEMP ligand 10 and analogues 11, 12, and 13 are the first examples of optically active bis(triarylphosphines) containing the axially dissymmetric biphenyl moiety.All these new diphosphines proved to be excellent asymmetry-inducing ligands in Rh(I)-catalyzed isomerizations of N,N-diethylnerylamine affording citronellal enamine of 98-99percent ee.
- Schmid, Rudolf,Cereghetti, Marco,Heiser, Bernd,Schoenholzer, Peter,Hansen, Hans-Juergen
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p. 897 - 930
(2007/10/02)
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