65020-70-4Relevant academic research and scientific papers
Preparation of Imidazole Derivatives via Bisfunctionalization of Alkynes Catalyzed by Ruthenium Carbonyl
Chen, Yue-Peng,Gu, Ling-Hui,He, Ling,Luo, Yang,Ruan, Yi-Tong,Yang, Ze
, p. 3520 - 3528 (2019/09/07)
A one-step, oxidative bisfunctionalization of alkynes to generate cis -enediol diacetates catalyzed by ruthenium carbonyl (triruthenium dodecacarbonyl) is presented. The reaction was performed using the alkyne, (diacetoxyiodo)benzene, Ru 3 (CO) 12 as the catalyst, and toluene as the solvent at 100 °C to give the cis -enediol diacetates in up to 82percent yields. This method overcomes the shortcomings of existing methods, such as tedious reaction steps, substrate limitations, and the use of toxic reagents. Furthermore, the reaction of module cis -enediol diacetates with ammonium carbonate [(NH 4) 2 CO 3 ] in an alcohol solvent gave imidazole derivatives in 37-84percent yields, thus providing a simple and mild new method for the synthesis of imidazole compounds.
PHARMACEUTICAL COMPOUNDS
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Page/Page column 28, (2012/03/27)
The invention relates to compounds and compositions for inhibiting the enzyme fatty acid amide hydrolase (FAAH), the use of the compounds in therapy and, in particular, for treating or preventing conditions whose development or symptoms are linked to subs
NONSTEROIDAL COMPOUNDS USEFUL AS MODULATORS OF GLUCOCORTICOID RECEPTOR AP-1 AND/OR NF-KAPPAB ACITIVITY AND USE THEREOF
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, (2011/11/06)
Disclosed are compounds of Formula (I) wherein: one of A and D is —N— and the other of A and D is —C—; or enantiomers, diastereomers, or pharmaceutically-acceptable salts thereof. Also disclosed are methods of using such compounds to modulate the function
Novel synthesis of the hexahydroimidazo[1,5b]isoquinoline scaffold: Application to the synthesis of glucocorticoid receptor modulators
Xiao, Hai-Yun,Wu, Dauh-Rurng,Malley, Mary F.,Gougoutas, Jack Z.,Habte, Sium F.,Cunningham, Mark D.,Somerville, John E.,Dodd, John H.,Barrish, Joel C.,Nadler, Steven G.,Dhar, T. G. Murali
experimental part, p. 1270 - 1280 (2010/08/05)
The first stereoselective synthesis of the hexahydroimidazo[1,5b] isoquinoline (HHII) scaffold as a surrogate for the steroidal A-B ring system is described. The structure-activity relationships of the analogs derived from this scaffold show that the basic imidazole moiety is tolerated by the glucocorticoid receptor (GR) in terms of binding affinity, although the partial agonist activity in the transrepressive assays depends on the substitution pattern on the B-ring.More importantly, most compounds in the HHII series bearing a tertiary alcohol moiety on the B-ring are either inactive or significantly less active in inducing GR-mediated transactivation, thus displaying a "dissociated" pharmacology in vitro. 2010 American Chemical Society.
Structure based development of phenylimidazole-derived inhibitors of indoleamine 2,3-dioxygenase
Kumar, Sanjeev,Jaller, Daniel,Patel, Bhumika,LaLonde, Judith M.,DuHadaway, James B.,Malachowski, William P.,Prendergast, George C.,Muller, Alexander J.
experimental part, p. 4968 - 4977 (2009/07/11)
Indoleamine 2,3-dioxygenase (IDO) is emerging as an important new therapeutic target for the treatment of cancer, chronic viral infections, and other diseases characterized by pathological immune suppression. With the goal of developing more potent IDO in
Imidazolylpyrimidine based CXCR2 chemokine receptor antagonists
Ho, Koc-Kan,Auld, Douglas S.,Bohnstedt, Adolph C.,Conti, Paolo,Dokter, Wim,Erickson, Shawn,Feng, Daming,Inglese, Jim,Kingsbury, Celia,Kultgen, Steven G.,Liu, Rong-Qiang,Masterson, Christopher M.,Ohlmeyer, Michael,Rong, Yajing,Rooseboom, Martijn,Roughton, Andrew,Samama, Philippe,Smit, Martin-Jan,Son, Ellen,van der Louw, Jaap,Vogel, Gerard,Webb, Maria,Wijkmans, Jac,You, Ming
, p. 2724 - 2728 (2007/10/03)
An imidazolylpyrimidine was identified in a CXCR2 chemokine receptor antagonist screen and was optimized for potency, in vitro metabolic stability, and oral bioavailability. It was found that subtle structural modification within the series affected the o
