190271-68-2Relevant articles and documents
Photochemical (Hetero-)Arylation of Aryl Sulfonium Salts
Zhao, Yue,Yu, Congjun,Liang, Wenjing,Patureau, Frederic W.
, p. 6232 - 6236 (2021/08/23)
The construction of (hetero)biaryls, which are ubiquitous scaffolds among medical substances, functional materials, and agrochemicals, constitutes a key application of cross-coupling methods. However, these usually require multiple synthetic steps. Herein, we report a simple photoinduced and catalyst-free C-H/C-H (hetero)arylation cross-coupling through aryl thianthrenium salts, which are formed site-selectively by direct C-H functionalization. The key to this approach is the UV-light, which can disrupt the C-S bond to form thianthrene radical cations and aryl radicals.
Discovery of an orally bioavailable NK1 receptor antagonist, (2s,3s)-(2- methoxy-5-tetrazol-1-ylbenzyl)(2-phenylpiperidin-3-yl)amine (GR203040), with potent antiemetic activity
Ward,Armour,Bays,Evans,Giblin,Heron,Hubbard,Liang,Middlemiss,Mordaunt,Naylor,Pegg,Vinader,Watson,Bountra,Evans
, p. 4985 - 4992 (2007/10/03)
The antiemetic, pharmacokinetic, and metabolic profile of CP-99,994, a potent NK1 receptor antagonist, has been carefully evaluated. As a result we began a medicinal chemistry program which initially identified a 3-furanyl analogue (6) with imp
