935520-36-8Relevant academic research and scientific papers
Arylation, Vinylation, and Alkynylation of Electron-Deficient (Hetero)arenes Using Iodonium Salts
Liu, Chuan,Wang, Qiu
supporting information, p. 5118 - 5121 (2016/10/14)
Arylation, vinylation, and alkynylation of electron-deficient arenes and heteroarenes have been achieved by chemoselective C-H zincation followed by copper-catalyzed coupling reactions using iodonium salts. This approach offers a direct and general access to a wide scope of (hetero)biaryls as well as alkenylated and alkynylated heteroarenes under mild conditions. It is particularly useful and valuable for the rapid and modular synthesis of diverse (hetero)aryl compounds, as demonstrated in the synthesis of transient receptor potential vanilloid 1 (TRPV1) antagonists and angiotensin II receptor type 1 (AT1 receptor) antagonists.
2-Aryl substituted pyridine C-region analogues of 2-(3-fluoro-4- methylsulfonylaminophenyl)propanamides as highly potent TRPV1 antagonists
Ryu, Hyungchul,Seo, Sejin,Kim, Myeong Seop,Kim, Mi-Yeon,Kim, Ho Shin,Ann, Jihyae,Tran, Phuong-Thao,Hoang, Van-Hai,Byun, Jieun,Cui, Minghua,Son, Karam,Sharma, Pankaz Kumar,Choi, Sun,Blumberg, Peter M.,Frank-Foltyn, Robert,Bahrenberg, Gregor,Koegel, Babette-Yvonne,Christoph, Thomas,Frormann, Sven,Lee, Jeewoo
, p. 4044 - 4047 (2014/09/03)
A series of 2-aryl pyridine C-region derivatives of 2-(3-fluoro-4- methylsulfonylaminophenyl)propanamides were investigated as hTRPV1 antagonists. Multiple compounds showed highly potent TRPV1 antagonism toward capsaicin comparable to previous lead 7. Among them, compound 9 demonstrated anti-allodynia in a mouse neuropathic pain model and blocked capsaicin-induced hypothermia in a dose-dependent manner. Docking analysis of 9 with our hTRPV1 homology model provided insight into its specific binding mode.
NOVEL VANILLOID RECEPTOR LIGANDS AND USE THEREOF FOR THE PRODUCTION OF PHARMACEUTICAL PREPARATIONS
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Page/Page column 144, (2010/11/27)
The present invention relates to novel vanilloid receptor ligands, to a process for the production thereof, to pharmaceutical preparations containing these compounds and to the use of these compounds for the production of pharmaceutical preparations.
