18463-71-3Relevant academic research and scientific papers
Synthesis of Functionalized Indolines and Dihydrobenzofurans by Iron and Copper Catalyzed Aryl C-N and C-O Bond Formation
Henry, Martyn C.,Senn, Hans Martin,Sutherland, Andrew
, p. 346 - 364 (2019/01/08)
A simple and effective one-pot, two-step intramolecular aryl C-N and C-O bond forming process for the preparation of a wide range of benzo-fused heterocyclic scaffolds using iron and copper catalysis is described. Activated aryl rings were subjected to a highly regioselective, iron(III) triflimide-catalyzed iodination, followed by a copper(I)-catalyzed intramolecular N-or O-arylation step leading to indolines, dihydrobenzofurans, and six-membered analogues. The general applicability and functional group tolerance of this method were exemplified by the total synthesis of the neolignan natural product, (+)-obtusafuran. DFT calculations using Fukui functions were also performed, providing a molecular orbital rationale for the highly regioselective arene iodination process.
[18F]MALEIMIDE-BASED GLYCOGEN SYNTHASE KINASE-3BETA LIGANDS FOR POSITRON EMISSION TOMOGRAPHY IMAGING AND RADIOSYNTHESIS METHOD
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Page/Page column 66, (2018/08/03)
The present invention provides a compound having the structure: (Formula I), and a method of inhibiting Glycogen synthase kinase-3 β (GSK-3β) in a subject comprising administering to the subject said compound, so as to thereby inhibit the GSK-3β in the subject.
Development of [18F]Maleimide-Based Glycogen Synthase Kinase-3β Ligands for Positron Emission Tomography Imaging
Hu, Kongzhen,Patnaik, Debasis,Collier, Thomas Lee,Lee, Katarzyna N.,Gao, Han,Swoyer, Matthew R.,Rotstein, Benjamin H.,Krishnan, Hema S.,Liang, Steven H.,Wang, Jin,Yan, Zhiqiang,Hooker, Jacob M.,Vasdev, Neil,Haggarty, Stephen J.,Ngai, Ming-Yu
, p. 287 - 292 (2017/03/17)
Dysregulation of glycogen synthase kinase-3β (GSK-3β) is implicated in the pathogenesis of neurodegenerative and psychiatric disorders. Thus, development of GSK-3β radiotracers for positron emission tomography (PET) imaging is of paramount importance, because such a noninvasive imaging technique would allow better understanding of the link between the activity of GSK-3β and central nervous system disorders in living organisms, and it would enable early detection of the enzyme’s aberrant activity. Herein, we report the synthesis and biological evaluation of a series of fluorine-substituted maleimide derivatives that are high-affinity GSK-3β inhibitors. Radiosynthesis of a potential GSK-3β tracer [18F]10a is achieved. Preliminary in vivo PET imaging studies in rodents show moderate brain uptake, although no saturable binding was observed in the brain. Further refinement of the lead scaffold to develop potent [18F]-labeled GSK-3 radiotracers for PET imaging of the central nervous system is warranted.
Pd(OAc)2-catalyzed lactonization of arylacetamides involving oxidation of C-H bonds
Uemura, Takeshi,Igarashi, Takuya,Noguchi, Moe,Shibata, Kaname,Chatani, Naoto
, p. 621 - 623 (2015/05/20)
The reaction of arylacetamides that contain a quinolin-8-ylmethylamine as the directing group with PhI(OAc)2, in the presence of Pd(OAc)2 as the catalyst, results in lactonization to give γ-lactones, the formation of which involves activation of the ortho C-H bonds, with concomitant cleavage of the directing group.
Synthesis, characterization and cardioprotective activity of some novel benzotriazole and pyrazole derivatives
Gudaparthi, Vijayalakshmi,Bharathi,Panda, Jagadeesh
, p. 5323 - 5330 (2012/07/28)
A series of N-(1-(1H-benzo[d]) [1,2,3]triazol-1-yl)-2,2-dimethyl propyl)-2-(substituted phenyl) acetamide derivatives and methyl 5-((4- (2,5-disubstituted phenyl) furan-2 carboxylate derivatives are prepared from different substituted aryl carboxylic acids, phenyl acetic acid and cinnamic acid, respectively. All the synthesized compounds are investigated for cardioprotective activity by ischemia reperfusion method, while all the compounds show significant activity.
A novel synthesis of aryl mesylates via one-pot demethylation-mesylation of aryl methyl ethers using a mixture of phosphorus pentoxide in methanesulfonic acid
Kaboudin, Babak,Abedi, Yaghoub
experimental part, p. 2025 - 2028 (2009/12/26)
A simple, efficient, and new method has been developed for the synthesis of aryl mesylates via one-pot demethylation-mesylation of aryl methyl ethers. Treatment of a variety of aryl methyl ethers with a mixture of phosphorus pentoxide in methanesulfonic a
3,4-DISUBSTITUTED MALEIMIDES FOR USE AS VASCULAR DAMAGING AGENTS
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Page/Page column 38, (2008/06/13)
This invention relates to novel compounds of Formula (I) for use as vascular damaging agents: Formula (I) wherein Rl, R7, R8, R9, ARI, AR2, AR3, p, q and r are as described in the specification. The invention also relates to methods for preparing compounds of Formula (I), to their use as medicaments (including methods for the treatment of angiogenesis or disease states associated with angiogenesis) and to pharmaceutical compositions containing compounds of Formula (I).
Mild oxidative one-carbon homologation of aldehyde to amide
Bonne, Damien,Dekhane, Mouloud,Zhu, Jieping
, p. 6926 - 6927 (2007/10/03)
One-carbon homologation of aldehyde into amide is realized in one-pot by its reaction with potassium α-p-methoxyphenyl-α-isocyano acetic acid (1c) and hydrochloride salt of dimethylamine (3a) in toluene at room temperature followed by acidic workup. In this multicomponent reaction, 1c served as donor of the CONH2 function to aldehyde, while the dimethylamine acted as a shuttle molecule to initiate/terminate the sequence and to mediate the internal redox process of one of the three-component adducts. Ready accessibility, nominal cost of the reagents, and mild conditions are attractive features of the present method. Copyright
ANTIULCER BENZIMIDAZOLE DERIVATIVES
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, (2008/06/13)
Compounds of formula I STR1 in which R 1 and R 2, which may be the same or different, are hydrogen, a C 1 to C 3 alkyl group or R 1 and R 2 together with the nitrogen to which they are attached form an optionally substituted heterocyclic ring; R 3 and R. sub.4, which may be the same or different are hydrogen, a C 1 to C. sub.3 alkyl or an optionally substituted C 3 to C 6 cycloalkyl group, or R 3 and R 4 together with the nitrogen to which they are attached form an optionally substituted heterocyclic ring; m is 0, 1 or 2; p is 0, 1 or 2; E is an alkylene group connected to or interrupted by an oxygen or a sulphur atom; J is hydrogen or a substituent group; and their pharmaceutically acceptable salts have utility as histamine H 2-receptor antagonists.
