Results 51 to 60 of about 5,024 (202)

Bromide-assisted chemoselective Heck reaction of 3-bromoindazoles under high-speed ball-milling conditions: synthesis of axitinib

open access: yesBeilstein Journal of Organic Chemistry, 2018
A mechanically-activated chemoselective Heck coupling for the synthesis of 3-vinylindazoles has been developed with the aid of catalytic amounts of TBAB and NaBr as both dehalogenation restrainer and grinding auxiliary.
Jingbo Yu   +5 more
doaj   +1 more source

Syntheses of 1-Aryl-5-nitro-1H-indazoles and a General One-Pot Route to 1-Aryl-1H-indazoles

open access: yesMolecules, 2018
An efficient route to substituted 1-aryl-1H-indazoles has been developed and optimized. The method involved the preparation of arylhydrazones from acetophenone or benzaldehyde substituted by fluorine at C2 and nitro at C5, followed by deprotonation and ...
Joel K. Annor-Gyamfi   +2 more
doaj   +1 more source

1,3-Dipolar cycloadditions of azomethine imines [PDF]

open access: yes, 2015
Azomethine imines are considered 1,3-dipoles of the aza-allyl type which are transient intermediates and should be generated in situ but can also be stable and isolable compounds.
Nájera, Carmen   +2 more
core   +3 more sources

Aplicação de α-oxoceteno ditiocetais em síntese orgânica Reactivity of α-oxoketene dithiocetals in organic synthesis

open access: yesQuímica Nova, 2010
The synthesis and reactivity of α-oxoketenes dithioacetals (S,S-acetals), general structure [(R¹C=OC(R²)=C(SR³)(SR4)], are reported. We also showed the application of S,S acetals as synthons for efficient synthesis of isoxazoles, pyrazoles ...
Geonir M. Siqueira   +5 more
doaj   +1 more source

Identification of novel 2-benzoxazolinone derivatives with specific inhibitory activity against the HIV-1 nucleocapsid protein [PDF]

open access: yes, 2018
In this report, we present a new benzoxazole derivative endowed with inhibitory activity against the HIV-1 nucleocapsid protein (NC). NC is a 55-residue basic protein with nucleic acid chaperone properties, which has emerged as a novel and potential ...
Botta, Maurizio   +9 more
core   +3 more sources

Multitarget drugs as potential therapeutic agents for alzheimer’s disease. A new family of 5-substituted indazole derivatives as cholinergic and BACE1 inhibitors

open access: yesJournal of Enzyme Inhibition and Medicinal Chemistry, 2022
Multitarget drugs are a promising therapeutic approach against Alzheimer’s disease. In this work, a new family of 5-substituted indazole derivatives with a multitarget profile including cholinesterase and BACE1 inhibition is described.
Pedro González-Naranjo   +9 more
doaj   +1 more source

An Efficient Protocol for Synthesis of Pyrazolo[3,4-a]acridines [PDF]

open access: yes, 2015
A new class of pyrazolo[3,4-a]acridines have been prepared, the synthon acridones were obtained in very good yield by one pot reaction of 2-amino-5-chloro or nitro substituted benzophenones with 1,3-cyclic diketones in the presence of freshly prepared ...
Kaminsky, Werner   +3 more
core   +2 more sources

Identification of an active metabolite of PAR-1 antagonist RWJ-58259 and synthesis of analogues to enhance its metabolic stability [PDF]

open access: yes, 2016
The discontinuation of PAR-1 antagonist RWJ-58259 beyond use as a biological probe is most likely due to it's short half-life in vivo. However, retention of significant in vivo activity beyond the point where most of the RWJ-58259 had been consumed ...
Caddick, S   +6 more
core   +1 more source

Suzuki-Type Cross-Coupling Reaction of Unprotected 3-Iodoindazoles with Pinacol Vinyl Boronate: An Expeditive C-3 Vinylation of Indazoles under Microwave Irradiation

open access: yesMolecules, 2018
Herein we report an expeditive C-3 vinylation of unprotected 3-iodoindazoles under microwave irradiation. Ten C-5 substituted 3-vinylindazole derivatives, nine of them novel, were synthesized through this method, which proceeds in moderate to excellent ...
Gonzalo Vera   +3 more
doaj   +1 more source

Discovery of potent and selective 5-azaindazole inhibitors of leucine-rich repeat kinase 2 (LRRK2) - Part 1 [PDF]

open access: yes, 2019
Parkinson’s disease is a relatively common neurological disorder with incidence increasing with age. Present treatments merely alleviate the symptoms and do not alter the course of the disease, thus identification of disease modifying therapies ...
Alessi, Dario   +8 more
core   +3 more sources

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