840526-76-3Relevant academic research and scientific papers
An efficient and recyclable ligand-free PEG1000-DIL/toluene temperature-dependent biphasic system for palladium catalysed Heck reactions
Liu, Xiang,Yao, Kai,Hu, Yu-Lin,Lu, Ming
experimental part, p. 731 - 733 (2012/03/10)
The Heck reaction of aryl halides with terminal olefins was successfully performed by using Pd (OAc)2 as the catalyst in a ligand-free PEG1000-DIL (PEG1000-based dicationic ionic liquid)/toluene system exhibiting temperature-dependent biphasic behavior. In addition, the isolation of the products is readily performed by a simply decantation, and the catalytic system can be recycled and reused without loss of catalytic activity.
Discovery of potent, orally available vanilloid receptor-1 antagonists. Structure-activity relationship of N-aryl cinnamides
Doherty, Elizabeth M.,Fotsch, Christopher,Bo, Yunxin,Chakrabarti, Partha P.,Chen, Ning,Gavva, Narender,Han, Nianhe,Kelly, Michael G.,Kincaid, John,Klionsky, Lana,Liu, Qingyian,Ognyanov, Vassil I.,Tamir, Rami,Wang, Xianghong,Zhu, Jiawang,Norman, Mark H.,Treanor, James J. S.
, p. 71 - 90 (2007/10/03)
The vanilloid receptor-1 (TRPV1 or VR1) is a member of the transient receptor potential (TRP) family of ion channels and plays a role in regulating the function of sensory nerves. A growing body of evidence demonstrates the therapeutic potential of TRPV1 modulators, particularly in the management of pain. As a result of our screening efforts, we identified (E)-3-(4-tert- butylphenyl)-N-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)acrylamide (1), an antagonist that blocks the capsaicin-induced and pH-induced uptake of 45Ca2+ in TRPV1-expressing Chinese hamster ovary cells with IC50 values of 17 ± 5 and 150 ± 80 nM, respectively. In this report, we describe the synthesis and structure-activity relationship of a series of N-aryl cinnamides, the most potent of which (49a and 49b) exhibit good oral bioavailability in rats (Foral = 39% and 17%, respectively).
Vanilloid receptor ligands and their use in treatments
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Page/Page column 34, (2008/06/13)
Compounds having the general structure and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache,
