857560-57-7Relevant academic research and scientific papers
An unexpected synthesis and application of ethyl 2,4-bis(chloromethyl)-6-iodoquinoline-3-carboxylate
Li, Yang,Dong, Shiyu,Tang, Bingyue,Zou, Hongtao,Jiang, Wenting
, p. 2215 - 2228 (2020)
An unexpected and direct synthesis of ethyl 2,4-bis(chloromethyl)-6-iodoquinoline-3-carboxylate (3) from the chlorotrimethylsilane (TMSCl)-promoted Friedl?nder reaction between 1-(2-amino-5-iodophenyl)ethanone (2) and ethyl 4-chloro-3-oxobutanoate has bee
Synthesis, structure, carbohydrate enzyme inhibition, antioxidant activity, in silico drug-receptor interactions and drug-like profiling of the 5-styryl-2-aminochalcone hybrids
Agbo, Emmanuel Ndubuisi,Choong, Yee Siew,Mphahlele, Malose J.
, (2021)
The 2-amino-5-(3/4-fluorostyryl)acetophenones were prepared and reacted with benzalde-hyde derivatives to afford the corresponding 5-styryl-2-aminochalcone hybrids. The trans geometry of the styryl and α,β-unsaturated carbonyl arms, and the presence of NH… O intramolecular hydrogen bond were validated using1 H-NMR and X-ray data. The 2-amino-5-styrylacetophenones and their 5-styryl-2-aminochalcone derivatives were screened in vitro for their capability to inhibit α-glucosidase and/or α-amylase activities. Their antioxidant properties were evaluated in vitro through the 2,2-diphenyl-1-picrylhydrazyl (DPPH) and nitric oxide (NO) free radical scavenging assays. Kinetic studies of the most active derivatives from each series against α-glucosidase and/or α-amylase activities have been performed supported by molecular docking studies to determine plausible protein–ligand interactions on a molecular level. The key aspects of the pharmacokinetics of these compounds, i.e., absorption, distribution, metabolism, and excretion have also been simulated at theoretical level. The most active compounds from each series, namely, 2a and 3e, were evaluated for cytotoxicity against the normal monkey kidney cells (Vero cells) and the adenocarcinomic human epithelial (A549) cell line to establish their safety profile at least in vitro.
A Convenient Formal [4+2] Heterocylization Route to Bis(triflyl)tetrahydroquinolines
Lázaro-Milla, Carlos,Almendros, Pedro
supporting information, p. 13534 - 13538 (2021/08/13)
We report the sustainable and efficient synthesis of a new type of quinoline derivatives bearing one or two SO2CF3 groups. The protocol is metal-, catalyst- and irradiation-free, involves the use of readily available and stable precursors, and avoids the formation of side products. Also, the mild conditions of the process allow the tolerance of a wide range of functional groups.
Silver(I)-catalyzed iodination of arenes: Tuning the lewis acidity of N-iodosuccinimide activation
Racys, Daugirdas T.,Sharif, Salaheddin A. I.,Pimlott, Sally L.,Sutherland, Andrew
, p. 772 - 780 (2016/02/18)
A mild and rapid method for the iodination of arenes that utilizes silver(I) triflimide as a catalyst for activation of N-iodosuccinimide has been developed. The transformation was found to be general for a wide range of anisole, aniline, acetanilide, and phenol derivatives and allowed the late-stage iodination of biologically active compounds such as PIMBA, a SPECT imaging agent of breast cancer, and (a?)-IBZM, a dopamine D2 receptor antagonist. The method was also modified for the radioiodination of arenes using a one-pot procedure involving the in situ generation of [125I]-N-iodosuccinimide followed by the silver(I)-catalyzed iodination.
Synthesis of 3-Substituted 2,1-Benzisoxazoles by the Oxidative Cyclization of 2-Aminoacylbenzenes with Oxone
Chiarini, Marco,Del Vecchio, Luana,Marinelli, Fabio,Rossi, Leucio,Arcadi, Antonio
, p. 3017 - 3030 (2016/10/12)
An efficient approach to the synthesis of 2,1-benzisoxazoles through direct construction of the N-O bond by the chemoselective oxidation of 2-aminoacylbenzenes with Oxone is described. This alternative methodology is characterized by its simple and transition-metal-free conditions and good functional group compatibility utilizing Oxone as a green oxidant instead of hypervalent iodine compounds. Moreover, this new procedure simplifies the number of steps compared to the previously reported procedure by circumventing the use of 2-azido-substituted aryl ketones.
Concise synthesis of 1-naphthols under mild conditions through a copper-catalyzed arylation of methyl ketones
Lou, Zhenbang,Zhang, Shu,Chen, Chao,Pang, Xinlong,Li, Ming,Wen, Lirong
supporting information, p. 153 - 159 (2014/03/21)
A concise synthesis of 1-naphthols via cyclization of o-iodoacetophenones and methyl ketones has been realized under very mild conditions. The cyclization process is initiated by a rare coppercatalyzed arylation of simple methyl ketones with ortho-iodoacetophenones.
CYCLOHEXYL-AZETIDINYL ANTAGONISTS OF CCR2
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Page/Page column 201-202, (2012/01/06)
The present invention comprises compounds of Formula (I). Wherein: R1, R2, R4, J, Q, and A are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I).
BIOSYNTHETICALLY GENERATED PYRROLINE-CARBOXY-LYSINE AND SITE SPECIFIC PROTEIN MODIFICATIONS VIA CHEMICAL DERIVATIZATION OF PYRROLINE-CARBOXY-LYSINE AND PYRROLYSINE RESIDUES
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Page/Page column 178, (2010/05/13)
Disclosed herein is pyrroline-carboxy-lysine (PCL), a pyrrolysine analogue, which is a natural, biosynthetically generated amino acid, and methods for biosynthetically generating PCL. Also disclosed herein are proteins, polypeptides and peptides that have PCL incorporated therein and methods for incorporating PCL into such proteins, polypeptides and peptides. Also disclosed herein is the site-specific derivatization of proteins, polypeptides and peptides having PCL or pyrrolysine incorporated therein. Also disclosed herein is the crosslinking of proteins, polypeptides and peptides having PCL or pyrrolysine incorporated therein.
CINNOLINE COMPOUNDS AS INHIBITORS OF PHOSPHODIESTERASE TYPE IV (PDE4)
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Page/Page column 13; 55, (2010/11/27)
There are provided according to the invention novel compounds of formula (I).
