76029-50-0Relevant academic research and scientific papers
A New Dioxazolone for the Synthesis of 1,2-Aminoalcohols via Iridium(III)-Catalyzed C(sp3)?H Amidation
Antien, Kevin,Geraci, Andrea,Parmentier, Michael,Baudoin, Olivier
supporting information, p. 22948 - 22955 (2021/09/09)
Vicinal aminoalcohols are widespread structural motifs in bioactive molecules. We report the development of a new dioxazolone reagent containing a p-nitrophenyldifluoromethyl group, which 1. displays a good safety profile; 2. shows a remarkably high react
Copper-Catalyzed Domino Reactions for the Synthesis of Phenothiazines
Huang, Manna,Huang, Dongting,Zhu, Xinhai,Wan, Yiqian
supporting information, p. 4835 - 4839 (2015/08/03)
A method for the one-pot synthesis of phenothiazines from benzothiazoles and aryl ortho-dihalides was explored. Preliminary work on the mechanism of the reaction suggested that it follows a domino process, including the hydrolysis of benzothiazoles followed by C-S coupling and C-N coupling. The low loading of the catalyst system (5 mol-% for both copper and ligand), the mild experimental conditions (90 °C, 12 h), and the use of a green reaction medium make this synthesis very attractive to academia and industry. A copper-catalyzed domino reaction consisting of the hydrolysis of benzothiazoles followed by C-S and C-N couplings for the synthesis of phenothiazines from benzothiazoles and aryl ortho-dihalides is described. The low loading of the catalyst system, mild experimental conditions, and the use of polyethylene glycol as the solvent make this synthetic approach very attractive to academia and industry.
Oxime glucokinase activators
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Page/Page column 7, (2008/12/06)
Disclosed herein are pyrazole glucokinase activators of the formula (I): that are useful for the treatment of metabolic diseases and disorders.
Parasiticidal 2-alkoxy- and 2-aryloxyiminoalkyl trifluoromethanesulfonanilides
Ali, Abdelselam,Altamore, Timothy M.,Bliese, Marianne,Fisara, Petr,Liepa, Andris J.,Meyer, Adam G.,Nguyen, Oahn,Sargent, Roger M.,Sawutz, David G.,Winkler, David A.,Winzenberg, Kevin N.,Ziebell, Angela
, p. 252 - 255 (2008/12/20)
A series of novel 2-alkoxy- and 2-aryloxyiminoalkyl trifluoromethanesulfonanilide derivatives have shown significant in vitro parasiticidal activity against the ectoparasites Ctenocephalides felis and Rhipicephalus sanguineus. A number of these compounds also displayed significant in vitro endoparasite activity against the nematode Haemonchus contortus. Crown Copyright
Studies on anti-MRSA parenteral cephalosporins II. Synthesis and antibacterial activity of 7 β-[2-(5-Amino-1,2,4-thiadiazol-3-yl)- 2(Z)-alkoxyiminoacetamido]-3(substituted imidazo[1,2-b] pyridazinium-1-yl)methyl-3-cephem-4-carboxylates and related compounds
Ishikawa,Kamiyama,Matsunaga,Tawada,Iizawa,Okonogi,Miyake
, p. 1071 - 1085 (2007/10/03)
In an effort to discover a novel cefozopran (CZOP) derivative having excellent antibacterial activity against methicillin-resistant Staphylococcus aureus (MRSA), we performed chemical modification of the alkoxyimino moiety and imidazo[1,2-b]pyridazinium group of CZOP. Among the prepared compounds, the cyclopentyloxyimino derivative 7β-[2-(5- amino-1,2, 4-thiadiazol-3-yl)-2(Z) -cyclopentyloxyiminoacetamido] -3-(3,6-diaminoimidazo[1,2- b]pyridazinium-1-yl)methyl-3-cephem-4-carboxylate (20g) showed the most potent anti-MRSA activity, reflecting its high affinity (IC50=1.6μg/ml) for penicillin binding protein 2' (PBP2'), although its anti-MRSA activity was slightly inferior to that of vancomycin (VCM). In experimental systemic infection in mice, however, 20g showed activity comparable to that of VCM against MRSA. In addition, 20g showed activity similar or slightly inferior to that of CZOP against Pseudomonas aeruginosa both in vitro and in vivo. Considering its favorable antibacterial activity profile, 20g was considered to be the most promising CZOP derivative for further studies.
Synthesis and opioid activities of some naltrexone oxime ethers
Mavunkel, B. J.,Rzeszotarski, W. J.,Kaplita, P. V.,DeHaven-Hudkins, D. L.
, p. 659 - 666 (2007/10/02)
A series of alkyl, cycloalkyl, aryl, and aralkyl ethers of naltrexone oxime was prepared.The compounds were examined in binding assays for μ, δ, and κ opioid receptor affinity.In addition, the naltrexone oxime ethers were studied in animal models that measure opioid agonist and antagonist activity.These studies led to the discovery of several compounds, notably phenethyl 3e and phenylpropyl 3f ethers of naltrexone, which have a 10-fold increase in potency at the κ opioid receptor with potent μ and κ agonist properties in vivo.naltrexone / oxime ether / opioid receptor / analgesia / receptor binding / kappa
