89943-04-4Relevant articles and documents
ADENOSINE RECEPTOR BINDING COMPOUNDS
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Paragraph 00421, (2020/02/06)
The present invention relates to pharmaceutical compounds and compositions of Formula (I) and methods of treatment using the compounds and compositions, especially for the treatment and/or prevention of a proliferation disorder, such as cancer. Compounds of Formula (I) as further described herein are shown modulators of the adenosine A2A receptor and exhibit antiproliferative activity. Accordingly, these compounds are useful to treat proliferative disorders such as cancer, and other adenosine receptor-related conditions including an inflammatory disease, renal disease, diabetes, vascular disease, lung disease, or an autoimmune disease.
An Improved Rapid and Mild Deoxygenation of Amine N-oxides
Rajesh
, p. 486 - 491 (2017/12/29)
An improved mild and selective method for the deoxygenation of a variety of amine N-oxides has been carried out in the presence of silica gel under mild conditions at room temperature to afford corresponding amines in relatively good yields without purification. The reaction is tolerant of a variety of functional groups such as hydroxyl, ester, acid, carbonyl, and cyano groups, as well as halogens. This method would be of great utility to synthesize various pyridines and amines easily.
Novel thermolabile protecting groups with higher stability at ambient temperature
Chmielewski, Marcin K.
supporting information; experimental part, p. 666 - 669 (2012/02/15)
Novel thermolabile hydroxyl protecting groups of increased thermostability are proposed. The stability of these groups at different temperatures ranges has been determined. The 2-pyridyl-N-(2,4-difluorobenzyl)aminoethyl unit was selected as stable at ambient temperature and very labile at increased temperature. The half-life times for the best groups were established. Application of this chemistry to the protection of different hydroxyl groups of thymidine was also demonstrated.
Engineering N-(2-pyridyl)aminoethyl alcohols as potential precursors of thermolabile protecting groups
Chmielewski, Marcin K.,Tykarska, Ewa,Markiewicz, Wojciech T.,Rypniewski, Wojciech
experimental part, p. 603 - 612 (2012/05/04)
Crystal and NMR analyses of four precursors of N-(2-pyridyl) thermolabile protecting group (TPG) were carried out. Two torsion angles have been identified as indicators that predict the molecules' thermolabile properties. Conformation that minimizes the N1...C8 distance is crucial for thermocyclisation. Nucleophilicity of the pyridyl ring is the driving force for the reaction but it is insufficient for thermocyclisation which is dominated by the molecules' ability to adopt a favourable conformation. The pKa value was recorded for all analyzed N-(2-pyridyl)aminoethyl alcohols. However, its effect is small in the determination of thermolability. Based on the analysis that we carried out, N-benzyl N-(2-pyridyl)aminoethyl was selected as a potential precursor of thermolabile carbonate of TPG. The Royal Society of Chemistry and the Centre National de la Recherche Scientifique 2012.
A mild, catalyst-free synthesis of 2-aminopyridines
Poola, Bhaskar,Choung, Wonken,Nantz, Michael H.
, p. 10798 - 10801 (2008/12/23)
Alkylation of 2-mercaptopyridine with 1,2-dibromoethane affords a cyclic dihydrothiazolopyridinium salt that can serve as a precursor of 2-aminopyridines. Its reaction with primary or secondary amines, either neat or in DMSO, under mild conditions gives the title compounds.
Synthesis of a β-strand mimetic based on a pyridine scaffold
Blomberg, David,Brickmann, Kay,Kihlberg, Jan
, p. 10937 - 10944 (2007/10/03)
A synthetic route to a 2,4-disubstituted pyridine as a potential β-strand mimetic has been developed and applied in the synthesis of a tripeptidomimetic of Leu-Gly-Gly. The pyridine scaffold replaces the central glycine, and is substituted with analogues
Amination of halopyridines on KF-alumina under microwave irradiation
Yang, De-Hong,Yang, Ben-Yong,Chen, Zhen-Chu,Chen, Song-Ying
, p. 600 - 601 (2007/10/03)
A convenient and clean synthesis of halopyridine-2-amines has been provided by amination of halopyridines on KF-alumina under microwave irradiation with good yields.
2,3-Dihydroimidazo[1,2-a]pyridines: A new class of enantioselective acyl transfer catalysts and their use in kinetic resolution of alcohols
Birman, Vladimir B.,Uffman, Eric W.,Jiang, Hui,Li, Ximin,Kilbane, Corey J.
, p. 12226 - 12227 (2007/10/03)
The long-known, but previously unexplored 2,3-dihydroimidazo[1,2-a]pyridine (DHIP) has been shown to be a competent acyl transfer catalyst. Its chiral 2-phenyl derivatives obtainable in two steps from commercially available starting materials have proved to be effective acylation catalysts, giving high levels of enantioselectivity (s = 20-85) in kinetic resolution of secondary benzylic alcohols. A transition state model explaining the observed selectivity has been proposed. Copyright
Pyridinium N-,(2'-azinyl)aminides: Regioselective synthesis of 2- alkylaminoazines
Martínez-Barrasa, Valentín,Delgado, Francisca,Burgos, Carolina,Luis García-Navío,Luisa Izquierdo,Alvarez-Builla, Julio
, p. 2481 - 2490 (2007/10/03)
The regioselective alkylation of pyridinium-N-(2f'-azinil)aminides with alkyl halides under mild conditions is described. The alkylation, combined with a reduction of the N-N bond, allows an easy preparation of 2- alkylaminoazines. (C) 2000 Elsevier Science Ltd.
