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.
Synthesis of 2,5-thiazole butanoic acids as potent and selective αvβ3 integrin receptor antagonists with improved oral pharmacokinetic properties
Wendt, John A.,Wu, Hongwei,Stenmark, Heather G.,Boys, Mark L.,Downs, Victoria L.,Penning, Thomas D.,Chen, Barbara B.,Wang, Yaping,Duffin, Tiffany,Finn, Mary Beth,Keene, Jeffery L.,Engleman, V. Wayne,Freeman, Sandra K.,Hanneke, Melanie L.,Shannon, Kristen E.,Nickols, Maureen A.,Steininger, Christina N.,Westlin, Marissa,Klover, Jon A.,Westlin, William,Nickols, G. Allen,Russell, Mark A.
, p. 845 - 849 (2007/10/03)
We describe a series of 2,5 thiazole containing compounds, which are potent antagonists of the integrin αvβ3 and show selectivity relative to the other integrins, such as αIIbβ 3 and αvβ6. These analogs were demonstrated to have high bioavailability relative to other relative heterocyclic analogs.
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
THIAZOLE COMPOUNDS AS INTEGRIN RECEPTOR ANTAGONISTS DERIVATIVES
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Page 68-69, (2008/06/13)
The present invention relates to pharmaceutical compositions comprising compounds of the Formula (I), and methods of selectively inhibiting or antagonizing the ανβ3 and/or the ανβ5 integrin without significantly inhibiting the ανβ6 integrin.
