177948-71-9Relevant academic research and scientific papers
Nickel-Catalyzed Reduction of Secondary and Tertiary Amides
Simmons, Bryan J.,Hoffmann, Marie,Hwang, Jaeyeon,Jackl, Moritz K.,Garg, Neil K.
supporting information, p. 1910 - 1913 (2017/04/11)
The nickel-catalyzed reduction of secondary and tertiary amides to give amine products is reported. The transformation is tolerant of extensive variation with respect to the amide substrate, proceeds in the presence of esters and epimerizable stereocenters, and can be used to achieve the reduction of lactams. Moreover, this methodology provides a simple tactic for accessing medicinally relevant α-deuterated amines.
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.
