816458-60-3Relevant articles and documents
Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 ((DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687)
Barlind, Jonas G.,Bauer, Udo A.,Birch, Alan M.,Birtles, Susan,Buckett, Linda K.,Butlin, Roger J.,Davies, Robert D.M.,Eriksson, Jan W.,Hammond, Clare D.,Hovland, Ragnar,Johannesson, Petra,Johansson, Magnus J.,Kemmitt, Paul D.,Lindmark, Bo T.,Morentin Gutierrez, Pablo,Noeske, Tobias A.,Nordin, Andreas,O'Donnell, Charles J.,Petersson, Annika U.,Redzic, Alma,Turnbull, Andrew V.,Vinblad, Johanna
, p. 10610 - 10629 (2013/02/23)
A new series of pyrazinecarboxamide DGAT1 inhibitors was designed to address the need for a candidate drug with good potency, selectivity, and physical and DMPK properties combined with a low predicted dose in man. Rational design and optimization of this series led to the discovery of compound 30 (AZD7687), which met the project objectives for potency, selectivity, in particular over ACAT1, solubility, and preclinical PK profiles. This compound showed the anticipated excellent pharmacokinetic properties in human volunteers.
N-H insertion reactions of Boc-amino acid amides: Solution- and solid-phase synthesis of pyrazinones and pyrazines
Matsushita, Hana,Lee, Sang-Hyeup,Yoshida, Kazuhiro,Clapham, Bruce,Koch, Guido,Zimmermann, Juerg,Janda, Kim D.
, p. 4627 - 4629 (2007/10/03)
(Chemical equation presented) A series of α-diazo-β-ketoesters were reacted with Boc amino acid amides in the presence of rhodium octanoate catalyst. The resulting N-H insertion products were treated with acid, providing the 1,4-azine intermediates, which
