19730-12-2Relevant academic research and scientific papers
Zirconium Catalyzed Hydroaminoalkylation for the Synthesis of α-Arylated Amines and N-Heterocycles
Koperniku, Ana,Schafer, Laurel L.
supporting information, p. 6334 - 6339 (2021/03/08)
The zirconium catalyzed hydroaminoalkylation of alkenes with N-aryl- and sterically demanding N-alkyl-α-arylated secondary amines by using commercially available Zr(NMe2)4 is reported. N-phenyl- and N-isopropylbenzylamine are used as amine substrates to establish the alkene substrate scope. Exclusively linear products are obtained in the presence of bulky vinylsilanes. Challenging α-heteroarylated amines and functionalized alkene substrates are compatible with this easy to use catalyst, affording a new disconnection strategy for the atom- and step-economic preparation of selectively substituted saturated α-arylated heterocycles.
Discovery of 5-phenoxy-1,3-dimethyl-1H-pyrazole-4-carboxamides as potent agonists of TGR5 via sequential combinatorial libraries
Londregan, Allyn T.,Piotrowski, David W.,Futatsugi, Kentaro,Warmus, Joseph S.,Boehm, Markus,Carpino, Philip A.,Chin, Janice E.,Janssen, Ann M.,Roush, Nicole S.,Buxton, Joanne,Hinchey, Terri
, p. 1407 - 1411 (2013/03/14)
Optimization of a high-throughput screening hit led to the discovery of a new series of 5-phenoxy-1,3-dimethyl-1H-pyrazole-4-carboxamides as highly potent agonists of TGR5. This novel chemotype was rapidly developed through iterative combinatorial library synthesis. It was determined that in vitro agonist potency correlated with functional activity data from human peripheral blood monocytes.
