3078-07-7Relevant articles and documents
1,3-dipolar cycloaddition of hydrazones with α-oxo-ketenes: A three-component stereoselective entry to pyrazolidinones and an original class of spirooxindoles
Presset, Marc,Mohanan, Kishor,Hamann, Marie,Coquerel, Yoann,Rodriguez, Jean
supporting information; experimental part, p. 4124 - 4127 (2011/10/04)
Stereodefined monocyclic, spirobicyclic, and bis-spirotricyclic pyrazolidin-3-ones can be prepared efficiently by a three-component reaction involving a 1,3-dipolar cycloaddition of azomethine imines obtained from hydrazones with α-oxo-ketene dipolarophiles generated in situ. The reaction allows the creation of four covalent bonds and two contiguous chiral quaternary centers with excellent diastereoselectivity in a single catalyst/additive-free, highly atom-economical transformation. From a fundamental point of view, the reaction introduces α-oxo-ketenes as effective dipolarophiles in 1,3-dipolar cycloadditions.
Isosteric ramatroban analogs: Selective and potent CRTH-2 antagonists
Robarge, Michael J.,Bom, David C.,Tumey, L. Nathan,Varga, Norbert,Gleason, Elizabeth,Silver, Daniel,Song, Jianping,Murphy, Steven M.,Ekema, George,Doucette, Chris,Hanniford, Doug,Palmer, Marc,Pawlowski, Gary,Danzig, Joel,Loftus, Margaret,Hunady, Karen,Sherf, Bruce A.,Mays, Robert W.,Stricker-Krongrad, Alain,Brunden, Kurt R.,Harrington, John J.,Bennani, Youssef L.
, p. 1749 - 1753 (2007/10/03)
The chemoattractant receptor-homologous molecule expressed on T H2 cells (CRTH-2), also found on eosinophils and basophils, is a prostaglandin D2 receptor involved in the recruitment of these cell types during an inflammatory response. In this report, we describe the synthesis and optimization of a ramatroban isostere that is a selective and potent antagonist of CRTH-2 which may be useful in the treatment of certain diseases.
