56446-64-1Relevant academic research and scientific papers
Ligand-Free Copper-Catalyzed Ullmann-Type C?O Bond Formation in Non-Innocent Deep Eutectic Solvents under Aerobic Conditions
Quivelli, Andrea Francesca,Marinò, Manuela,Vitale, Paola,García-álvarez, Joaquín,Perna, Filippo M.,Capriati, Vito
, (2021/12/09)
An efficient and novel protocol was developed for a Cu-catalyzed Ullmann-type aryl alkyl ether synthesis by reacting various (hetero)aryl halides (Cl, Br, I) with alcohols as active components of environmentally benign choline chloride-based eutectic mixtures. Under optimized conditions, the reaction proceeded under mild conditions (80 °C) in air, in the absence of additional ligands, with a catalyst [CuI or CuII species] loading up to 5 mol% and K2CO3 as the base, providing the desired aryloxy derivatives in up to 98 % yield. The potential application of the methodology was demonstrated in the valorization of cheap, easily available, and naturally occurring polyols (e. g., glycerol) for the synthesis of some pharmacologically active aryloxypropanediols (Guaiphenesin, Mephenesin, and Chlorphenesin) on a 2 g scale in 70–96 % yield. Catalyst, base, and deep eutectic solvent could easily and successfully be recycled up to seven times with an E-factor as low as 5.76.
PHENYL AMINO PIPERIDINE mTORC INHIBITORS AND USES THEREOF
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Paragraph 0475-0477, (2018/05/24)
The present invention provides compounds, compositions thereof, and methods of using the same.
THIAZOLIDINONE COMPOUNDS AND USE THEREOF
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Paragraph 1156-1157, (2017/09/21)
A pharmaceutical composition containing a compound of Formula (I) for treating an opioid receptor-associated condition. Also disclosed is a method for treating an opioid receptor-associated condition using such a compound. Further disclosed are two sets of thiazolidinone compounds of formula (I): (i) compounds each having an enantiomeric excess greater than 90% and (ii) compounds each being substituted with deuterium.
Acetylene-free synthesis of vinyloxy pyridine and quinoline
Hamdi, Abdelrahman,Mostafa, Amany S.,Watat, Cedric Nana,Laurent, Mathieu Y.,Ben Ayed, Kawther,Selim, Khalid B.,Dujardin, Gilles
supporting information, p. 5825 - 5829 (2016/12/06)
Copper-catalyzed vinylation of 2- and 4-hydroxy pyridine and quinoline affords exclusively N-vinylation products. However, vinyl ethers of 4-hydroxy pyridine and quinoline can be prepared via a three-step sequence involving copper-catalyzed C-O cross coupling reaction of the corresponding N-heteroaryl bromides with ethylene glycol, chlorination of the terminal alcohol, and dehydrohalogenation of the β-chloro ethers. Although not efficient in 2-hydroxy series, this method can be conveniently applied to the preparation of various aza-aryl vinyl ethers in moderate to good overall yields.
PROBES FOR IMAGING HUNTINGTIN PROTEIN
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Paragraph 0275, (2016/03/22)
Provided are imaging agents comprising a compound of Formula (I), or a pharmaceutically acceptable salt thereof, and methods of their use.
N-SUBSTITUTED BENZIMIDAZOLYL C-KIT INHIBITORS
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Page/Page column 57-58, (2008/06/13)
Compounds represented by Formula (I): or a pharmaceutically acceptable salt or N-oxide thereof, are useful in the treatment of cancer.
Amination of aryl halides using copper catalysis
Lang, Fengrui,Zewge, Daniel,Houpis, Ioannis N.,Volante
, p. 3251 - 3254 (2007/10/03)
Bromopyridine 4 was converted into aminopyridine 5 under Cu2O catalysis with an ethylene glycol solution of ammonia in excellent yield (90%). The amination reaction features low (0.5 mol%) catalyst loading, mild reaction temperature (80°C) and low reaction pressure (50 psi). This protocol is further studied in the amination of a variety of aryl halides.
