84199-61-1Relevant academic research and scientific papers
Metal-free visible light-promoted synthesis of isothiazoles: A catalytic approach for N-S bond formation from iminyl radicals under batch and flow conditions
Alemán, José,Berton, Mateo,Cabrera-Afonso, María Jesús,Cembellín, Sara,Halima-Salem, Adnane,Maestro, M. Carmen,Marzo, Leyre,Miloudi, Abdellah
supporting information, p. 6792 - 6797 (2020/11/09)
A sustainable synthesis of isothiazoles has been developed using an α-amino-oxy acid auxiliary and applying photoredox catalysis. This simple strategy features mild conditions, broad scope and wide functional group tolerance representing a new enviromenta
Approach to 5-substituted 6,7,8,9-tetrahydro-5H-pyrido[3,2-c]azepines
Subota, Andrii I.,Artamonov, Oleksiy S.,Gorlova, Alina,Volochnyuk, Dmitriy M.,Grygorenko, Oleksandr O.
supporting information, p. 1989 - 1991 (2017/04/27)
An approach to 5-substituted 6,7,8,9-tetrahydro-5H-pyrido[3,2-c]azepines via the cyclization of 1-(2-(3-azidopropyl)pyridin-3-yl)alkanones under Staudinger–aza-Wittig reaction conditions is described. The overall reaction sequence includes eight steps and allows for the preparation of gram quantities of the title products. In some cases, the formation of 5,7,8,9-tetrahydrooxepino[4,3-b]pyridine derivatives was observed.
One-Pot Asymmetric Synthesis of Alkylidene 1-Alkylindan-1-ols Using Br?nsted Acid and Palladium Catalysis
Faggyas, Réka J.,Calder, Ewen D. D.,Wilson, Claire,Sutherland, Andrew
, p. 11585 - 11593 (2017/11/10)
A one-pot catalytic enantioselective allylboration/Mizoroki-Heck reaction of 2-bromoaryl ketones has been developed for the asymmetric synthesis of 3-methyleneindanes bearing a tertiary alcohol center. Br?nsted acid-catalyzed allylboration with a chiral BINOL derivative was followed by a palladium-catalyzed Mizoroki-Heck cyclization, resulting in selective formation of the exo-alkene. This novel protocol provides a concise and scalable approach to 1-alkyl-3-methyleneindan-1-ols in high enantiomeric ratios (up to 96:4 er). The potential of these compounds as chiral building blocks was demonstrated with efficient transformation to optically active diol and amino alcohol scaffolds.
THIAZOLE DERIVATIVES FOR THE TREATMENT OF ANIMAL TRYPANOSOMIASIS
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Page/Page column 74; 77, (2016/10/04)
The present invention relates to a novel class of compounds of general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, X and Y are as defined herein, to their use in human and veterinary medicine, and in the treatment of animal trypanosomiasis in particular, to compositions containing them, to processes for their preparation and to intermediates used in such processes.
Silver-catalysed intramolecular cyclisation of 2-alkynylacetophenones and 3-acetyl-2-alkynylpyridines in the presence of ammonia
Dell'Acqua, Monica,Abbiati, Giorgio,Arcadi, Antonio,Rossi, Elisabetta
scheme or table, p. 7836 - 7848 (2011/12/02)
Silver-catalysed/microwave-assisted domino reactions of 2-alkynyl-acetophenones and 3-acetyl-2-alkynylpyridines in the presence of ammonia are widely described. In most cases the reaction give a mixture of the imino- and carbo-cyclisation products, with a
Discovery, synthesis, and bioactivity of bis(heteroaryl)piperazines. 1. A novel class of non-nucleoside HIV-1 reverse transcriptase inhibitors
Romero,Morge,Biles,Berrios-Pena,May,Palmer,Johnson,Smith,Busso,Tan,Voorman,Reusser,Althaus,Downey,So,Resnick,Tarpley,Aristoff
, p. 999 - 1014 (2007/10/02)
A variety of analogues of 1-[4-methoxy-3,5-dimethylbenzyl]-4-[3- (ethylamino)-2-pyridyl]piperazine hydrochloride (U-80493E) were synthesized and evaluated for their inhibition of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase (RT). Replacement of the substituted aryl moiety with various substituted indoles provided bis(heteroaryl)piperazines (BHAPs) that were 10-100-fold more potent than U-80493E. The pyridyl portion of the lead molecule was found to be very sensitive to modifications. Extensive preclinical evaluations of several of these compounds led to the selection of 1-[(5-methoxyindol-2-yl)carbonyl]-4-[3-(ethylamino)-2- pyridyl]piperazine methanesulfonate (U-87201E, atevirdine mesylate) for clinical evaluation.
