199589-50-9Relevant articles and documents
Generation of gold carbenes in water: Efficient intermolecular trapping of the α-oxo gold carbenoids by indoles and anilines
Li, Long,Shu, Chao,Zhou, Bo,Yu, Yong-Fei,Xiao, Xin-Yu,Ye, Long-Wu
, p. 4057 - 4064 (2014/10/15)
The efficient intermolecular reaction of gold carbene intermediates, generated via gold-catalyzed alkyne oxidation, with indoles and anilines has been realized in aqueous media. Importantly, it was revealed for the first time that water could dramatically suppress the undesired over-oxidation, providing a general and practical solution to the problem of over-oxidation in gold-catalyzed intermolecular alkyne oxidation with external nucleophiles. This strategy was successfully applied to the formal synthesis of the Pfizer's chiral endothelin antagonist UK-350,926.
The design and synthesis of a novel series of indole derived selective ETA antagonists
Rawson, David J.,Dack, Kevin N.,Dickinson, Roger P.,James, Kim
, p. 125 - 128 (2007/10/03)
Conformational constraint has been used as the key design element in the identification of a series of potent and selective ETA antagonists. The most potent antagonist, 32, (ETA IC50 = 0.55 nM) is 722-fold selective over t