- Synthesis of crescent shaped heterocycle-fused aromatics via Garratt-Braverman cyclization and their DNA-binding studies
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Three crescent shaped heterocycle-fused phenanthrene based systems 1–3 have been synthesized starting from benzene (or substituted benzene) 1,2-bis-propargyl alcohols. Bis-alkylation with propargylic bromides provided the key intermediate, the bis-propargyl bis-ethers. In spite of the possibility of many competing reactions, the latter underwent facile double Garratt-Braverman cyclization to provide compounds 1–3 in near quantitative yield, in a striking reaction involving the formation of four C–C bonds in a single step. Compounds 1–3 showed binding interaction with DNA, predominantly, via groove binding along with partial intercalation (combilexins). Molecular docking study supported the proposed binding modes.
- Ghosh, Debaki,Basu, Souradeep,Singha, Monisha,Das, Joyee,Bhattacharya, Prabuddha,Basak, Amit
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p. 2014 - 2018
(2017/05/04)
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- Synthesis of 1,2-Bis(trifluoromethylthio)arenes via Aryne Intermediates
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A general method for synthesis of 1,2-bis-trifluoromethylthioarenes has been developed. Arynes generated from silyl aryl triflates or halides react with bis(trifluoromethyl)disulfide to afford 1,2-bis-trifluoromethylthioarenes. Aryl, alkyl, ester, halide,
- Mesgar, Milad,Daugulis, Olafs
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supporting information
p. 4247 - 4250
(2017/08/23)
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- Fused Amino Pyridines for the Treatment of Lung Cancer
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The present invention relates to the use of compounds with fused amino pyridine core for the treatment of malignancies associated with brain and lung. The oral administration of compounds of the instant application results in effective brain penetration and provides for non-intrusive treatment of brain and lung tumors.
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Paragraph 0159
(2016/11/17)
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- DEVICE AND METHOD FOR EVALUATING ORGANIC MATERIAL FOR ORGANIC SOLAR CELL
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Provided are a novel 1,2-bis(dialkylphosphino)-4,5-(methylenedioxy)benzene derivative that forms a metal complex having particularly high asymmetry induction capacity and catalytic activity on β-dehydroamino acids, a method for manufacturing the same, a metal complex having this 1,2-bis(dialkylphosphino)-4,5-(methylenedioxy)benzene derivative as a ligand, and an asymmetric hydrogenation method using this metal complex. A 1,2-bis(dialkylphosphino)-4,5-(methylenedioxy)benzene derivative represented by general formula (1). (In the formula, R1 and R2 represent an alkyl group having 1-10 carbon atoms, and R1 and R2 have different numbers of carbon atoms.)
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Paragraph 0059; 0060; 0061
(2014/08/07)
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- Aryne Insertion into I-I σ-Bonds
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A new protocol for the efficient synthesis of o-diiodoarenes has been developed. This method allows the synthesis of substituted and polycyclic o-diiodoarenes, which are difficult to obtain by classical methods. This diiodination process involves the formal insertion of arynes into the I-I σ-bond.
- Rodriguez-Lojo, Diego,Cobas, Agustin,Pena, Diego,Perez, Dolores,Guitian, Enrique
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supporting information; experimental part
p. 1363 - 1365
(2012/05/20)
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- Rigid P-chiral phosphine ligands with tert -butylmethylphosphino groups for rhodium-catalyzed asymmetric hydrogenation of functionalized alkenes
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Both enantiomers of 2,3-bis(tert-butylmethylphosphino)quinoxaline (QuinoxP*), 1,2-bis(tert-butylmethylphosphino)benzene (BenzP*), and 1,2-bis(tert-butylmethylphosphino)-4,5-(methylenedioxy)benzene (DioxyBenzP*) were prepared in short steps from enantiopure (S)- and (R)-tert-butylmethylphosphine-boranes as the key intermediates. All of these ligands were crystalline solids and were not readily oxidized on exposure to air. Their rhodium complexes exhibited excellent enantioselectivities and high catalytic activities in the asymmetric hydrogenation of functionalized alkenes, such as dehydroamino acid derivatives and enamides. The practical utility of these catalysts was demonstrated by the efficient preparation of several chiral pharmaceutical ingredients having an amino acid or a secondary amine component. A rhodium complex of the structurally simple ligand BenzP* was used for the mechanistic study of asymmetric hydrogenation. Low-temperature NMR studies together with DFT calculations using methyl α-acetamidocinnamate as the standard model substrate revealed new aspects of the reaction pathways and the enantioselection mechanism.
- Imamoto, Tsuneo,Tamura, Ken,Zhang, Zhenfeng,Horiuchi, Yumi,Sugiya, Masashi,Yoshida, Kazuhiro,Yanagisawa, Akira,Gridnev, Ilya D.
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supporting information; experimental part
p. 1754 - 1769
(2012/03/11)
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- Hypervalent iodine(III)-LiX combination in fluoroalcohol solvent for aromatic halogenation of electron-rich arenecarboxylic acids
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The novel reagent system, PhI(OAc)2-LiX combination in fluoroalcohol solvents, was found to be effective for halodecarboxylation of electron-rich arenecarboxylic acids. The method provided an efficient route to halogenated phenol ether derivatives. Georg Thieme Verlag Stuttgart ? New York.
- Hamamoto, Hiromi,Hattori, Sho,Takemaru, Kaori,Miki, Yasuyoshi
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scheme or table
p. 1563 - 1566
(2011/08/03)
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- COMPOUNDS AS HSP90 INHIBITORS
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The invention provides novel compounds of formula (I) wherein: one of the a, b, c or d members is a nitrogen atom and the remaining members are carbon atoms; and R3 is a radical selected from the group consisting of: —S—R14 and —CH2—R15. The compounds of formula (I) are useful for treating diseases mediated by a heat shock protein 90 (Hsp 90)
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Page/Page column 67
(2009/03/07)
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- FUSED AMINO PYRIDINE AS HSP90 INHIBITORS
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The present invention relates to HSP90 inhibitors containing fused amino pyridine core that are useful as inhibitors of HSP90 and their use in the treatment of HSP90 related diseases and disorders such as cancer, an autoimmune disease, or a neurodegenerative disease.
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Page/Page column 39
(2008/12/08)
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- Iodination of alkyl aryl ethers by mercury(II) oxide-iodine reagent in dichloromethane
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A convenient method for selective mono- and diiodination of alkyl aryl ethers by mercury(II) oxide-iodine reagent in dichloromethane is reported.
- Orito,Hatakeyama,Takeo,Suginome
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p. 1273 - 1277
(2007/10/02)
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