115109-77-8Relevant articles and documents
Palladium-catalyzed carbonylative cyclization of aryl alkenes/alkenols: A new reaction mode for the synthesis of electron-rich chromanes
Li, Shuang,Li, Fuzhuo,Gong, Jianxian,Yang, Zhen
supporting information, p. 1240 - 1243 (2015/03/14)
The Pd(II)-catalyzed intramolecular carbonylative cyclization reaction of aryl alkenes and aryl alkenols is reported for the synthesis of structurally diverse chromanes. PdCl2(CH3CN)2 was used as the catalyst and CuCl2 as the oxidant under the balloon pressure of CO. The reaction is conducted under mild conditions, and chromane-type esters and lactones can be generated in a highly regio- and stereoselective manner.
Novel benzo[1,4]diazepin-2-one derivatives as endothelin receptor antagonists
Bolli, Martin H.,Marfurt, Judith,Grisostomi, Corinna,Boss, Christoph,Binkert, Christoph,Hess, Patrick,Treiber, Alexander,Thorin, Eric,Morrison, Keith,Buchmann, Stephan,Bur, Daniel,Ramuz, Henri,Clozel, Martine,Fischli, Walter,Weller, Thomas
, p. 2776 - 2795 (2007/10/03)
Since its discovery in 1988 by Yanagisawa et al., endothelin (ET), a potent vasoconstrictor, has been widely implicated in the pathophysiology of cardiovascular, cerebrovascular, and renal diseases. Many research groups have embarked on the discovery and development of ET receptor antagonists for the treatment of such diseases. While several compounds, e.g., ambrisentan 2, are in late clinical trials for various indications, one compound (bosentan, Tracleer) is being marketed to treat pulmonary arterial hypertension. Inspired by the structure of ambrisentan 2, we designed a novel class of ET receptor antagonists based on a 1,3,4,5-tetrahydro-1H-benzo[e][1,4]diazepin-2-one scaffold. Here, we report on the preparation as well as the in vitro and in vivo structure-activity relationships of these derivatives. Potent dual ET A/ETB receptor antagonists with affinities in the low nanomolar range have been identified. In addition, several compounds efficiently reduced arterial blood pressure after oral administration to Dahl salt sensitive rats. In this animal model, the efficacy of the benzo[e] [1,4]diazepin-2-one derivative rac-39au was superior to that of racemic ambrisentan, rac-2.