7190-80-9Relevant academic research and scientific papers
Synthesis and bioevaluation of 6-chloropyridazin-3-yl hydrazones and 6-chloro-3-substituted-[1,2,4]triazolo[4,3-b]pyridazines as cytotoxic agents
Mamta,Aggarwal, Ranjana,Sadana, Rachna,Ilag, Jeziel,Sumran, Garima
, p. 288 - 295 (2019/02/12)
An efficient synthesis of a series of 6-chloro-3-substituted-[1,2,4]triazolo[4,3-b]pyridazines is described via intramolecular oxidative cyclization of various 6-chloropyridazin-3-yl hydrazones with iodobenzene diacetate. The structures of the newly synth
Electrochemical synthesis of 1,2,4-triazole-fused heterocycles
Ye, Zenghui,Ding, Mingruo,Wu, Yanqi,Li, Yong,Hua, Wenkai,Zhang, Fengzhi
supporting information, p. 1732 - 1737 (2018/04/30)
A reagent-free intramolecular dehydrogenative C-N cross-coupling reaction has been developed under mild electrolytic conditions. In this atom- and step-economical one-pot process, valuable 1,2,4-triazolo[4,3-a]pyridines and related heterocyclic compounds could be synthesized efficiently from commercially available aliphatic or (hetero)aromatic aldehydes and 2-hydrazinopyridines. Various functional groups are compatible with this metal- and oxidant-free protocol which can be carried out on a gram scale easily. This novel method was applied to the synthesis of one of the top-selling drugs Xanax and late stage functionalization for generating chemical diversity in biologically relevant lead molecules.
Synthesis method of 1,2,4-triazolohetercyclic compound
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Paragraph 0046; 0047, (2018/01/09)
The invention provides a method for synthesizing a 1,2,4-triazolohetercyclic compound. The method comprises the following steps: dissolving a 2-hydrazinohetercyclic compound (I) and an aldehyde compound (II) into acetonitrile A; stirring at 25 DEG C to 80
Synthesis of 1,2,4-Triazolo[4,3-a]pyridines and Related Heterocycles by Sequential Condensation and Iodine-Mediated Oxidative Cyclization
Li, Ertong,Hu, Zhiyuan,Song, Lina,Yu, Wenquan,Chang, Junbiao
, p. 11022 - 11027 (2016/07/27)
A facile and efficient approach to access 1,2,4-triazolo[4,3-a]pyridines and related heterocycles has been accomplished through condensation of readily available aryl hydrazines with corresponding aldehydes followed by iodine-mediated oxidative cyclizatio
Kinase domain inhibition of leucine rich repeat kinase 2 (LRRK2) using a [1,2,4]triazolo[4,3-b]pyridazine scaffold
Galatsis, Paul,Henderson, Jaclyn L.,Kormos, Bethany L.,Han, Seungil,Kurumbail, Ravi G.,Wager, Travis T.,Verhoest, Patrick R.,Noell, G. Stephen,Chen, Yi,Needle, Elie,Berger, Zdenek,Steyn, Stefanus J.,Houle, Christopher,Hirst, Warren D.
, p. 4132 - 4140 (2014/09/17)
Leucine rich repeat kinase 2 (LRRK2) has been genetically linked to Parkinson's disease (PD). The most common mutant, G2019S, increases kinase activity, thus LRRK2 kinase inhibitors are potentially useful in the treatment of PD. We herein disclose the str
Triazolopyridazine LRRK2 kinase inhibitors
Franzini, Maurizio,Ye, Xiaocong M.,Adler, Marc,Aubele, Danielle L.,Garofalo, Albert W.,Gauby, Shawn,Goldbach, Erich,Probst, Gary D.,Quinn, Kevin P.,Santiago, Pam,Sham, Hing L.,Tam, Danny,Truong, Anh,Ren, Zhao
, p. 1967 - 1973 (2013/04/24)
Leucine-rich repeat kinase 2 (LRRK2) has been implicated in the pathogenesis of Parkinson's disease (PD). Inhibition of LRRK2 kinase activity is a therapeutic approach that may lead to new treatments for PD. Herein we report the discovery of a series of [
Chemical studies on 3,6-dichloropyridazine (part 2)
El-Salam, N.M. Abd,Al Shoaibi,Ahmed
experimental part, p. 1944 - 1950 (2012/05/31)
3,6-Dichloropyridazine (1) reacted with 2-aminophenol, phenylalanine, acetophenone hydrazone derivatives, acid hydrazide derivatives and amino-aromatic acids (anthranilic acid and 5-bromoanthranilic acid) and yield the compounds (2), (3), (4a,b), (5a,b) a
Palladium-catalyzed coupling of aldehyde-derived hydrazones: Practical synthesis of triazolopyridines and related heterocycles
Thiel, Oliver R.,Achmatowicz, Michal M.,Reichelt, Andreas,Larsen, Robert D.
supporting information; experimental part, p. 8395 - 8398 (2010/12/25)
The palladium-catalyzed intermolecular coupling of aldehyde-derived hydrazones with chloroazines, followed by oxidative cyclization under mild conditions afforded access to a broad variety of bicyclic heterocyclic scaffolds (see scheme) that have potentia
MAOS protocols for the general synthesis and lead optimization of 3,6-disubstituted-[1,2,4]triazolo[4,3-b]pyridazines
Aldrich, Leslie N.,Lebois, Evan P.,Michelle Lewis,Nalywajko, Natalia T.,Niswender, Colleen M.,David Weaver,Jeffrey Conn,Lindsley, Craig W.
scheme or table, p. 212 - 215 (2009/05/07)
General, high-yielding MAOS protocols for the expedient synthesis of functionalized 3,6-disubstituted-[1,2,4]triazolo[4,3-b]pyridazines are described amenable to an iterative analog library synthesis strategy for the lead optimization of an M1 antagonist
