722549-99-7Relevant articles and documents
Streamlined Synthesis of Diaminopyridines by Pd-Catalyzed Ammonia Coupling with Deactivated Amino-Chloropyridines
Bourriquen, Florian,Bruneau-Voisine, Antoine,Jeandin, Aliénor,Stihle, Etienne,Fantasia, Serena
, p. 9006 - 9011 (2019/06/24)
An efficient and cost-effective two-step synthesis of diaminopyridines, fundamental building blocks of biologically active compounds, is reported. The advantages over previously reported routes include cost and wider availability of the bromo-chloropyridine starting materials and the straightforward accessibility to an extended array of diaminopyridine regioisomers. The key enabler of this synthetic strategy is the development of an unprecedented palladium-catalyzed coupling reaction of ammonia with chloropyridines deactivated by the presence of an alkylamino substituent. The coupling reaction was accomplished with very low catalyst loadings under remarkably mild reaction conditions, making the system particularly suitable for both academic and industrial applications. The utility of this methodology is exemplified by the application to the synthesis of highly relevant scaffolds, including the synthetic intermediates of the marketed drugs Ribociclib and Palbociclib.
Convergent, parallel synthesis of a series of β-substituted 1,2,4-oxadiazole butanoic acids as potent and selective α vβ3 receptor antagonists
Boys, Mark L.,Schretzman, Lori A.,Chandrakumar, Nizal S.,Tollefson, Michael B.,Mohler, Scott B.,Downs, Victoria L.,Penning, Thomas D.,Russell, Mark A.,Wendt, John A.,Chen, Barbara B.,Stenmark, Heather G.,Wu, Hongwei,Spangler, Dale P.,Clare, Michael,Desai, Bipin N.,Khanna, Ish K.,Nguyen, Maria N.,Duffin, Tiffany,Engleman, V. Wayne,Finn, Mary Beth,Freeman, Sandra K.,Hanneke, Melanie L.,Keene, Jeffery L.,Klover, Jon A.,Nickols, G. Allen,Nickols, Maureen A.,Steininger, Christina N.,Westlin, Marisa,Westlin, William,Yu, Yi X.,Wang, Yaping,Dalton, Christopher R.,Norring, Sarah A.
, p. 839 - 844 (2007/10/03)
We describe a series of 1,2,4-oxadiazoles, which are potent antagonists of the integrin αvβ3 and, in addition, show selectivity relative to the other β3 integrin αIIbβ3. In whole cells, the majority o
