53406-38-5Relevant academic research and scientific papers
Oxalohydrazide Ligands for Copper-Catalyzed C?O Coupling Reactions with High Turnover Numbers
Ray, Ritwika,Hartwig, John F.
supporting information, p. 8203 - 8211 (2021/03/08)
Here, we report a class of ligands based on oxalohydrazide cores and N-amino pyrrole and N-amino indole units that generates long-lived copper catalysts for couplings that form the C?O bonds in biaryl ethers. These Cu-catalyzed coupling of phenols with aryl bromides occurred with turnovers up to 8000, a value which is nearly two orders of magnitude higher than those of prior couplings to form biaryl ethers and nearly an order of magnitude higher than those of any prior copper-catalyzed coupling of aryl bromides and chlorides. This ligand also led to copper systems that catalyze the coupling of aryl chlorides with phenols and the coupling of aryl bromides and iodides with primary benzylic and aliphatic alcohols. A wide variety of functional groups including nitriles, halides, ethers, ketones, amines, esters, amides, vinylarenes, alcohols and boronic acid esters were tolerated, and reactions occurred with aryl bromides in pharmaceutically related structures.
1-[(Imidazolidin-2-yl)imino]-1H-indoles as new hypotensive agents: synthesis and in vitro and in vivo biological studies
Kornicka, Anita,Wasilewska, Aleksandra,S?czewski, Jaros?aw,Hudson, Alan L.,Boblewski, Konrad,Lehmann, Artur,Gzella, Karol,Belka, Mariusz,S?czewski, Franciszek,Gdaniec, Maria,Rybczyńska, Apolonia,B?czek, Tomasz
, p. 400 - 410 (2017/04/03)
A series of 1-[(imidazolidin-2-yl)imino]-1H-indole analogues of hypotensive α2-AR agonists, 1-[(imidazolidin-2-yl)imino]-1H-indazoles, was synthesized and tested in vitro for their activities at α1- and α2-adrenoceptors as well as imidazoline I1 and I2 receptors. The most active 1-[(imidazolidin-2-yl)imino]-1H-indoles displayed high or moderate affinities for α1- and α2-adrenoceptors and substantial selectivity for α2-adrenoceptors over imidazoline-I1 binding sites. The in vivo cardiovascular properties of indole derivatives 3 revealed that substitution at C-7 position of the indole ring may result in compounds with high cardiovascular activity. Among them, 7-fluoro congener 3g showed the most pronounced hypotensive and bradycardic activities in this experiment at a dose as low as 10?μg/kg i.v. Metabolic stability of the selected compounds of type 3 was determined using both in vitro and in silico approaches. The results indicated that these compounds are not vulnerable to rapid first-phase oxidative metabolism.
HETEROARYL COMPOUNDS FOR KINASE INHIBITION
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Paragraph 463, (2016/04/26)
Compounds and pharmaceutical compositions that modulate kinase activity, including mutant EGFR and mutant HER2 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including mutant EGFRand mutant HER2 activity, are described herein.
N-amination of indoles on pilot-plant scale via simultaneous and proportional metering of reagents
Weiberth, Franz J.,Hanna, Reda G.,Lee, George E.,Polverine, Yvonne,Klein, Joseph T.
experimental part, p. 704 - 709 (2011/12/04)
The N-amination of indoles on large scale, utilizing a portable Coriolis mass flow metering and pumping system that provides precise dispensing of two reagent streams simultaneously and proportionally, is described.
USE OF NEUROPROTECTIVE COMPOUNDS IN OBTAINING MEDICAMENTS INTENDED FOR THE TREATMENT OF NEURODEGENERATING DISEASES
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, (2009/12/23)
Use of neuroprotective compounds in obtaining medicaments intended for the curative treatment of neurodegenerative disease and/or the prevention of the appearance of disorders ensuing from those diseases.
1H-Indole-Pyridinecarboxamide and 1H-Indole-Piperidinecarboxamide Compounds
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Page/Page column 7, (2009/10/21)
Compounds of formula (I): wherein: A represents a divalent radical: wherein: Z represents an oxygen atom or a sulphur atom,R6 represents a hydrogen atom, an alkyl, alkenyl, arylalkyl or polyhaloalkyl group or a substituted, linear or branched alkyl chain, represents a single bond or a double bond,R1, R2, R3 and R4 represent a hydrogen or halogen atom,an alkyl, alkoxy, hydroxy, cyano, nitro, polyhaloalkyl or optionally substituted amino group, or a linear or branched alkyl chain substituted by one or more groups,R5 represents a hydrogen atom or an alkyl, aminoalkyl or hydroxyalkyl group,X and Y represent a hydrogen atom or an alkyl group,Ra, Rb, Rc and Rd represent a hydrogen or halogen atom, an alkyl, hydroxy, alkoxy, cyano, nitro, polyhaloalkyl, optionally substituted amino group, or a substituted, linear or branched alkyl chain,Re represents a hydrogen atom or an alkyl, arylalkyl or alkenyl group or a substituted, linear or branched alkyl chain, their enantiomers, diastereoisomers, and N-oxides, and also addition salts thereof with a pharmaceutically acceptable acid or base.
Naphthalocyanine dye and method for producing the same
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Page/Page column 18, (2008/06/13)
A compound of the following formula (I): wherein L11, L21, L31 and L41 represent a divalent group; Q11, Q21, Q31 and Q41 represent a non-metallic atomic group necessary for forming a hetero ring; R12, R22, R32 and R42 represent a substituent; n11, n12, n21, n22, n31, n32, n41 and n42 indicate an integer of from 0 to 6; provided that (n11+n21+n31+n41) is not 0; M1 represents two hydrogen atoms, two monovalent metal atoms, a divalent metal atom, or a divalent substituted metal atom including a trivalent or tetravalent metal atom.
Composition and antiviral activity of substituted azaindoleoxoacetic piperazine derivatives
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, (2008/06/13)
This invention provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with azaindoleoxoacetyl piperazine derivatives. These compounds possess unique antiv
Syntheses of novel indole lipoic acid derivatives and their antioxidant effects on lipid peroxidation
Gurkan, A. Selen,Karabay, Arzu,Buyukbingol, Zeliha,Adejare, Adeboye,Buyukbingol, Erdem
, p. 67 - 73 (2007/10/03)
The aim of the study was to examine antioxidant properties of conjugates based on indole and lipoic acid moieties. The design and syntheses of novel indole α-lipoic acid derivatives were performed. The antioxidant properties of target compounds were investigated using rat liver microsomal, NADPH-dependent lipid peroxidation inhibition. Some of the target compounds, especially those containing amide linker at position 5 of indole ring, proved to be highly effective in inhibiting lipid peroxidation as compared to α-lipoic acid.
PROCESS FOR THE PREPARATION OF N-AMINO SUBSTITUTED HETEROCYCLIC COMPOUNDS
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Page/Page column 22; 25; 26, (2008/06/13)
An improved process for the preparation of N-amino nitrogen heterocyclic compounds is disclosed and claimed. In an ambodiment of this invention, a compound of the formula (VI) is prepared starting from the corresponding indole derivative by way of N-amination and subsequently forming an hydrazone by the reaction with a keto compound in a single step. Further reduction of the hydrazone and subsequent coupling with a pyridine compound affords the compound of formula VI or a suitable salt thereof.
