255060-79-8Relevant academic research and scientific papers
Enantioselective synthesis of cyclic sulfamidates by using chiral rhodium-catalyzed asymmetric transfer hydrogenation
Kang, Soyeong,Han, Juae,Lee, Eun Sil,Choi, Eun Bok,Lee, Hyeon-Kyu
supporting information; experimental part, p. 4184 - 4187 (2010/11/19)
Asymmetric transfer hydrogenation (ATH) of cyclic sulfamidate imines 4 and 9, using a HCO2H/Et3N mixture as the hydrogen source and well-defined chiral Rh catalysts (S,S)- or (R,R)-2, CpRhCl(TsDPEN), effectively produces the corresponding cyclic sulfamidates with excellent yields and enantioselectivities at room temperature within 0.5 h. ATH of 4,5-disubstituted imines 9, having preexisting stereogenic centers, is shown to take place with dynamic kinetic resolution.
Highly potent inhibitors of TNF-α production. Part II: Metabolic stabilization of a newly found chemical lead and conformational analysis of an active diastereoisomer
Matsui, Toshiaki,Kondo, Takashi,Nishita, Yoshitaka,Itadani, Satoshi,Tsuruta, Hiroshi,Fujita, Setsuko,Omawari, Nagashige,Sakai, Masaru,Nakazawa, Shuichi,Ogata, Akihito,Mori, Hideaki,Kamoshima, Wataru,Terai, Kouichiro,Ohno, Hiroyuki,Obata, Takaaki,Nakai, Hisao,Toda, Masaaki
, p. 3787 - 3805 (2007/10/03)
Design and synthesis of metabolically stabilized inhibitors of TNF-α production, which could be new drug candidates, are reported. Conformational analysis of an active diastereoisomer was performed based on biological evaluations of the conformationally f
Additions of Enantiopure α-Sulfinyl Carbanions to (S)-N-Sulfinimines: Asymmetric Synthesis of β-Amino Sulfoxides and β-Amino Alcohols
Garcia Ruano, Jose L.,Alcudia, Ana,Del Prado, Miriam,Barros, David,Carmen Maestro,Fernandez, Inmaculada
, p. 2856 - 2862 (2007/10/03)
The addition of the lithium anions derived from (R)- and (S)-methyl and -ethyl p-tolyl sulfoxides to (S)-N-benzylidene-p-toluenesulfinamide provides an easy access route to enantiomerically pure β-(N-sulfinyl)amino sulfoxides. Stereoselectivity can be ach
3-[3-(piperidin-1-yl)propyl]indoles as highly selective h5-HT(1D) receptor agonists
Russell, Michael G. N.,Matassa, Victor G.,Pengilley, Roy R.,Van Niel, Monique B.,Sohal, Bindi,Watt, Alan P.,Hitzel, Laure,Beer, Margaret S.,Stanton, Josephine A.,Broughton, Howard B.,Castro, José L.
, p. 4981 - 5001 (2007/10/03)
Several 5-HT(ID/1B) receptor agonists are now entering the marketplace as treatments for migraine. This paper describes the development of selective h5-HT(1D)receptor agonists as potential antimigraine agents which may produce fewer side effects. A series of 3-[3-(piperidin-1-yl)propyl]indoles has been synthesized which has led to the identification of 80 (L-772,405), a high- affinity h5-HT(1D) receptor full agonist having 170-fold selectivity for h5- HT(1D) receptors over h5-HT(1B) receptors. L-772,405 also shows very good selectivity over a range of other serotonin and nonserotonin receptors and has excellent bioavailability following subcutaneous administration in rats. It therefore constitutes a valuable tool to delineate the role of h5-HT(1D) receptors in migraine. Molecular modeling and physical properties have been utilized to postulate the binding conformation of these compounds in the receptor cavity.
