90868-93-2Relevant academic research and scientific papers
Nickel(II)- And Silver(I)-Catalyzed C-H Bond Halogenation of Anilides and Carbamates
Kianmehr, Ebrahim,Afaridoun, Hadi
, p. 1513 - 1523 (2020/12/14)
ortho -C-H bond halogenation of anilides and N -aryl carbamates using easily available N -halosuccinimides (NXS) as the active halogenation reagent in the presence of nickel or silver catalyst has been developed. This method provides a new approach to 2-haloanilides and carbamates, which may serve as starting materials for the synthesis of pharmaceutically and biologically active compounds.
Discovery of Novel Indole Derivatives as Fructose-1,6-bisphosphatase Inhibitors and X-ray Cocrystal Structures Analysis
Ji, Wenming,Liu, Quan,Liu, Shuainan,Shen, Zhufang,Wang, Xiaoyu,Xu, Bailing,Zhao, Linxiang,Zhao, Rui,Zhou, Jie
supporting information, (2022/01/03)
Liver fructose-1,6-bisphosphatase (FBPase) is a key enzyme in the gluconeogenesis, and its inhibitors are expected to be novel antidiabetic agents. Herein, a series of new indole and benzofuran analogues were designed and synthesized to evaluate the inhib
Monoprotected l-Amino Acid (l-MPAA), Accelerated Bromination, Chlorination, and Iodination of C(sp2)?H Bonds by Iridium(III) Catalysis
Kathiravan, Subban,Nicholls, Ian A.
supporting information, p. 7031 - 7036 (2017/05/29)
Halogenated arenes are important structural motifs commonly found in biologically active molecules and used for a variety of transformations in organic synthesis. Herein, we report the mono-protected l-amino acid (l-MPAA) accelerated iridium(III)-catalyzed halogenation of (hetero)anilides at room temperature. This reaction constitutes the first example of an iridium(III)/l-MPAA-catalyzed general halogenation of (hetero)arenes through C(sp2)?H activation. Furthermore, we demonstrate the potential utility of our method through its use in the synthesis of a quinolone derivative.
Novel acid-type cyclooxygenase-2 inhibitors: Design, synthesis, and structure-activity relationship for anti-inflammatory drug
Hayashi, Shigeo,Ueno, Naomi,Murase, Akio,Nakagawa, Yoko,Takada, Junji
experimental part, p. 179 - 195 (2012/07/27)
Cyclooxygenase (COX) is a key rate-limiting enzyme for prostaglandin (PG) production cascades in the human body. The mechanisms of both the anti-inflammation effects and the side-effects of traditional COX inhibitors are associated with the existence of two COX isoforms. Thus while COX-1 is predominantly expressed ubiquitously and constitutively, and it serves a housekeeping role in processes such as gastrointestinal (GI) mucosa protection, COX-2 is absent or exhibits a low level of expression in most tissues, and is highly upregulated in response to endotoxin, virus, inflammatory or tissue-injury stimuli/signals, and tumour promoter in the various types of organs, tissues, and cells. Furthermore, COX-2 contribution to PGE2 and PGI2 production evokes and sustains systemic or peripheral inflammatory disease, but it is not involved in the COX-1-mediated GI tract events. Also, hypersensitivity of aspirin owing to its inhibitory action against COX-1 is a significant concern clinically. Consequently, highly selective COX-2 inhibitors have been needed for the treatment of inflammatory- and inflammation related-diseases that include pyrexia, inflammation, pain, rheumatoid arthritis, osteoarthritis, and cancers. In this study, a series of novel [2-{[(4-substituted or 4,5-disubstituted)-pyridin-2-yl]carbonyl}-(5- or 6-substituted or 5,6-disubstituted)-1H-indol-3-yl]acetic acid analogues was designed, synthesized, and evaluated to identify potent and selective COX-2 inhibitors as potential agents against inflammatory diseases. As significant findings, the present study clarified unique structure-activity relationship of the analogues toward potent and selective COX-2 inhibition in vitro, and identified 2-{6-fluoro-2-[4-methyl-2-pridinyl)carbonyl]-1H-indol-3-yl}acetic acid as a potent and selective COX-2 inhibitor in vitro that demonstrated orally potent anti-inflammation efficacy against carrageenan-induced oedema formation in the foot of SPF/VAF male SD rats as a peripheral inflammation model in vivo.
A simple synthetic protocol for oxidation of alkyl-arenes into ketones using a combination of HBr-H2O2
Khan, Abu T.,Parvin, Tasneem,Choudhury, Lokman H.,Ghosh, Subrata
, p. 2271 - 2274 (2007/10/03)
A wide variety of alkyl- and cycloalkyl-arenes undergo benzylic C-H oxidation by employing a combination of 48% hydrogen bromide and 30% hydrogen peroxide in dichloromethane at room temperature. In addition, a chemoselective oxidation at the benzylic position is feasible by deactivating the aromatic ring using the same combination.
Convenient strategies for the preparation of modified 2(3H)-benzothiazolethiones
Chaudhuri, Narayan C.
, p. 3783 - 3790 (2007/10/03)
4-Alkyl-2-bromoanilines and 4-alkoxy-2-chloroanilines were synthesized conveniently and submitted to cyclization reaction with potassium O-ethyl dithiocarbonate to afford 6-substituted 2(3H)-benzothiazolethiones in good yields.
