- INHIBITORS OF PURINE NUCLEOSIDE PHOSPHORYLASE - SYNTHESIS AND USE THEREOF FOR TREATMENT OF T-CELL ACUTE LYMPHOBLASTIC LEUKEMIA AND LYMPHOMA
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The present invention relates to new compounds of general formula I, their synthesis, their pharmaceutically acceptable salts, and their use in treatment of T-cell acute lymphoblastic leukemia and lymphoma.
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- Iodolopyrazolium Salts: Synthesis, Derivatizations, and Applications
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The synthesis of iodolopyrazolium triflates via an oxidative cyclization of 3-(2-iodophenyl)-1H-pyrazoles is described. The reaction is characterized by a broad substrate scope, and various applications of these novel cyclic iodolium salts acting as useful synthetic intermediates are demonstrated, in particular in site-selective ring openings. This was finally applied to generate derivatives of the anti-inflammatory drug celecoxib. Their application as highly active halogen-bond donors is shown as well.
- Boelke, Andreas,Caspers, Lucien D.,Kuczmera, Thomas J.,Lork, Enno,Nachtsheim, Boris J.
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p. 7261 - 7266
(2020/10/05)
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- One-Pot Synthesis and Conformational Analysis of Six-Membered Cyclic Iodonium Salts
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Two one-pot procedures for the construction of carbon-bridged diaryliodonium triflates and tetrafluoroborates are described. Strong Br?nsted acids enable the effective Friedel-Crafts alkylation with diversely substituted o-iodobenzyl alcohol derivatives, providing diphenylmethane scaffolds, which are subsequently oxidized and cyclized to the corresponding dibenzo[b,e]iodininium salts. Based on NMR investigations and density functional theory (DFT) calculations, we could verify the so-far-undescribed existence of two stable isomers in cyclic iodonium salts substituted with aliphatic side chains in the carbon bridge.
- Caspers, Lucien D.,Spils, Julian,Damrath, Mattis,Lork, Enno,Nachtsheim, Boris J.
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p. 9161 - 9178
(2020/08/14)
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- ISOQUINOLINE DERIVATIVES AS PERK INHIBITORS
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The invention is directed to substituted isoquinoline derivatives and uses thereof. Specifically, the invention is directed to compounds according to Formula I and the use of compounds of Formula (I) in treating disease states: (I) wherein R1,
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- Cu-Catalyzed Enantioselective Ring Opening of Cyclic Diaryliodoniums toward the Synthesis of Chiral Diarylmethanes
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A Cu-catalyzed enantioselective desymmetrizing ring-opening reaction of six-membered cyclic diaryliodonium salts with carboxylic acids or thioacids is reported for the facile access to chiral diarylmethanes. A Cu/[cyclopropyl bis(oxazoline)] catalyst well
- Li, Bin,Chao, Zengyin,Li, Chunyu,Gu, Zhenhua
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p. 9400 - 9403
(2018/07/30)
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- Intramolecular Pd-Catalyzed Arylation of 1-Amidosugars: A New Route to N-Glycosyl Quinolin-2-ones
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The synthesis of N-glycosylated quinolin-2-ones via an intramolecular N-arylation of glycosylamides is reported. The coupling involves the use of only Pd(OAc)2 as the catalyst and nBu4NOAc as the base in 1,4-dioxane. This versatile approach allows the synthesis of various N-glycosylated quinolin-2-ones with exclusive α or β selectivity.
- Luong, Thi Thanh Huyen,Brion, Jean-Daniel,Lescop, Ewen,Alami, Mouad,Messaoudi, Samir
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p. 2126 - 2129
(2016/06/01)
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- Intriguing substituent effect in modified Hoveyda-Grubbs metathesis catalysts incorporating a chelating iodo-benzylidene ligand
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A series of modified Hoveyda-Grubbs catalysts incorporating a chelating iodo-benzylidene ligand were prepared and characterized. The presence of electron-withdrawing ring substituents in the para position to the iodide was found to decrease the catalytic activity, revealing that dissociation of the Ru...I-Ar bond is not the rate-determining step.
- Barbasiewicz, Michal,Blocki, Krzysztof,Malinska, Maura,Pawlowski, Robert
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supporting information
p. 355 - 358
(2013/02/22)
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- Palladium-catalyzed insertion of N-tosylhydrazones for the synthesis of isoindolines
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Isoindolines are synthesized by palladium-catalyzed coupling reaction of N-(2-iodobenzyl) anilines with α,β-unsaturated N-tosylhydrazones. The reaction has several potential advantages: (1) toleration of a wide range of functional groups, (2) easy to handle and with mild conditions, (3) enriches the isoindoline family, (4) two new bonds form in one step.
- Zhou, Ping-Xin,Luo, Jian-Yi,Zhao, Lian-Biao,Ye, Yu-Ying,Liang, Yong-Min
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p. 3254 - 3256
(2013/05/08)
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- Functionalized dibenzoborepins as components of small molecule and polymeric π-conjugated electronic materials
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We present the synthesis and characterization of dibenzo[b,f]borepins (DBBs) functionalized at the para and meta position with respect to the boron center in order to understand how regiochemical issues influence photophysical and electrochemical properti
- Caruso, Anthony,Tovar, John D.
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p. 2227 - 2239
(2011/06/11)
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- BORON-CONTAINING PI-ELECTRON MATERIALS INCORPORATING FORMALLY AROMATIC AND NEUTRAL BOREPIN RINGS
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The synthesis, functionalization and characterization of borepin-based extended pi-electron molecules is disclosed. Bulky substituents shielded the vacant boron p-orbitals thus allowing synthetic manipulation and purification under ambient lab conditions.
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- OPE/OPV H-mers: Synthesis, electronic properties, and spectroscopic responses to binding with transition metal ions
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A new type of structurally defined H-shaped OPE/OPV co-oligomers (termed H-mers) functionalized with various donor and/or acceptor end groups was synthesized by iterative Sonogashira coupling and Horner-Wadsworth-Emmons (HWE) reactions. Electronic substitution effects on the H-mer backbone were investigated by UV-vis absorption and fluorescence spectroscopy. Some H-mers were found to show spectral responses upon binding to an acid (TFA) or transition metal ions, revealing the applicability of H-mers in the field of chromophore and fluorophore based chemosensors.
- Zhou, Ningzhang,Wang, Li,Thompson, David W.,Zhao, Yuming
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p. 125 - 143
(2011/03/17)
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- H-shaped OPE/OPV oligomers: A new member of 2D-conjugated fluorophore cores
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(Chemical Equation Presented) A new class of two-dimensional (2D), π-conjugated, skewed H-shaped co-oligomers of phenylene vinylene and phenylene ethynylene (11a-d, termed H-mers) were synthesized using Sonogashira coupling and Wittig-Horner reactions as the key steps. Electronic and spectroscopic properties of the H-mers were investigated by UV-vis absorption, fluorescence spectroscopic techniques, and ab initio calculations (HF/3-21G). Two amino-containing functional H-mers (11b and 11d) were found to exhibit appealing fluorescence sensitivity to selected Bronsted acids and transition-metal ions.
- Zhou, Ningzhang,Wang, Li,Thompson, David W.,Zhao, Yuming
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supporting information; experimental part
p. 3001 - 3004
(2009/04/18)
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- Bicyclic-substituted amines having cyclic-substituted monocyclic substituents
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Compounds of formula (I) wherein R1 or R2 is an aromatic or non-aromatic ring directly joined or joined by a linker, as represented by L2 and L3, to a heteroaromatic core, and X, X′, Y, Y′, Z, Z′, R1,
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Page/Page column 18-19
(2010/02/14)
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- Tri-and bi-cyclic heteroaryl histamine-3 receptor ligands
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Compounds of formula (I) wherein R1 or R2 is a tricyclic or bicyclic ring, each of which contains at least two heteroatoms, and R1, R2, R3, R3a, R3b, R4, R5, L, X, X′, Y, Y′, Z, and Z′ are as defined herein, are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands, methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).
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Page/Page column 20; 21; 36
(2010/02/14)
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- Bicyclic-substituted amines having cyclic-substituted monocyclic substituents
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Compounds of formula (I) wherein R1 or R2 is an aromatic or non-aromatic ring directly joined or joined by a linker, as represented by L2 and L3, to a heteroaromatic core, and X, X′, Y, Y′, Z, Z′, R1,
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Page/Page column 19-20
(2010/02/14)
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- Tri- and bi-cyclic heteroaryl histamine-3 receptor ligands
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Compounds of formula (I) wherein R1 or R2 is a tricyclic or bicyclic ring, each of which contains at least two heteroatoms, and R1, R2, R3, R3a, R3b, R4, R5
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Page/Page column 20; 36
(2010/02/14)
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- Bicyclic-substituted amines as histamine-3 receptor ligands
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Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands and methods for using such comp
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Page/Page column 19-20; 46
(2008/06/13)
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