162398-65-4Relevant academic research and scientific papers
Copper(ii)-catalyzed c-n coupling of aryl halides and n-nucleophiles promoted by quebrachitol or diethylene glycol
Chen, Guoliang,Chen, Yuanguang,Du, Fangyu,Fu, Yang,Wu, Ying,Zhou, Qifan
supporting information, p. 2161 - 2168 (2019/11/25)
Herein, we report the natural ligand quebrachitol (QCT) as a promoter for a Cu(II) catalyst, which is highly effective for N-Arylation of various amines and related aryl halides. A series of diarylamine derivatives were obtained in high yields by using diethylene glycol (DEG) as both ligand and solvent. The C-N coupling reactions proceed under mild conditions and exhibit good functional group tolerance.
Photo/nickel synergistic catalysis method for monoarylation of diol
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Paragraph 0043; 0056-0059, (2018/09/13)
The invention discloses a photo/nickel synergistic catalysis method for monoarylation of a diol. The method directly uses a brominated aromatic hydrocarbon and a diol as raw materials, wherein the brominated aromatic hydrocarbon and the diol are simple and easy to obtain, and adopts a BODIPY organic photosensitizer and an inexpensive nickel source to synergistically catalyze cross-coupling of thediol and the brominated aromatic hydrocarbon without an additionally-added ligand to realize selective monoarylation of a diol compound, and a mono/dual arylation ratio is up to 18:1. The method disclosed by the invention has good tolerance of functional groups and is suitable for a plurality of diol compounds with different structures, such as o-diol, 1,3-diol, 1,4-diol and monodisperse polyethylene glycol; more importantly, the photosensitizer used in the method has a low using amount, the reaction temperature is close to room temperature, and the method is green, economical and highly-efficient; and the advantages make the method have higher scale synthetic value and can serve social and economic development.
Discovery of potent inhibitors of human and mouse fatty acid amide hydrolases
Butini, Stefania,Brindisi, Margherita,Gemma, Sandra,Minetti, Patrizia,Cabri, Walter,Gallo, Grazia,Vincenti, Silvia,Talamonti, Emanuela,Borsini, Franco,Caprioli, Antonio,Stasi, Maria Antonietta,Di Serio, Stefano,Ros, Sindu,Borrelli, Giuseppe,Maramai, Samuele,Fezza, Filomena,Campiani, Giuseppe,MacCarrone, Mauro
experimental part, p. 6898 - 6915 (2012/09/22)
Fatty acid amide hydrolase (FAAH, EC 3.5.1.99) is the main enzyme catabolizing endocannabinoid fatty acid amides. FAAH inactivation promotes beneficial effects upon pain and anxiety without the side effects accompanying agonists of type-1 cannabinoid receptors. Aiming at discovering new selective FAAH inhibitors, we developed a series of compounds (5a-u) characterized by a functionalized heteroaromatic scaffold. Particularly, 5c and 5d were identified as extremely potent, noncompetitive, and reversible FAAH inhibitors endowed with a remarkable selectivity profile and lacking interaction with the hERG channels. In vivo antinociceptive activity was demonstrated for 5c, 5d, and 5n at a dose much lower than that able to induce either striatal and limbic stereotypies or anxiolytic activity, thus outlining their potential to turn into optimum preclinical candidates. Aiming at improving pharmacokinetic properties and metabolic stability of 5d, we developed a subset of nanomolar dialyzable FAAH inhibitors (5v-z), functionalized by specific polyethereal lateral chains and fluorinated aromatic rings.
Synthesis of oxygen-substituted N-alkyl 1-deoxynojirimycin derivatives: aza sugar &α-glucosidase inhibitors showing antiviral (HIV-1) and immunosuppressive activity
Broek, L. A. G. M. van den,Vermaas, D. J.,Kemenade, F. J. van,Tan, M. C. C. A.,Rotteveel, F. T. M.,et al.
, p. 507 - 516 (2007/10/02)
The synthesis of a series of six less-lipophilic analogues of the α-glucosidase inhibitor N-decyl-1-deoxynojirimycin (N-decyl-dNM, 5) is described.With the incorporation of a single oxygen atom, particularly at position seven in the N-decyl side-chain to
