70122-89-3Relevant articles and documents
High yielding allylation of a chiral secondary alcohol containing base sensitive functional groups
Kraus, James M.,Gits, Hunter C.,Silverman, Richard B.
, p. 1319 - 1322 (2012)
Inhibitors of neuronal nitric oxide synthase, based on a chiral pyrrolidine scaffold, show promise for the treatment of certain neurodegenerative diseases. We recently reported the synthesis of a series of selective inhibitors, but the method was limited at a key step of forming an allyl ether intermediate. Yields for this step were very inconsistent, and the presence of base sensitive functional groups limited the range of available methods for forming this ether bond. This work describes a novel application of palladium catalyzed decarboxylative allylation, consistently resulting in a 90% isolated yield, which is crucial for the synthesis of this critical late stage intermediate. We also report a new quantitative yielding and straightforward synthesis of the allyl-t-butylcarbonate precursor.
Structure-based design, synthesis and bioactivity evaluation of macrocyclic inhibitors of mutant isocitrate dehydrogenase 2 (IDH2) displaying activity in acute myeloid leukemia cells
Che, Jinxin,Chen, Binhui,Dong, Xiaowu,Gao, Anhui,Gao, Jian,Hu, Xiaobei,Hu, Yongzhou,Huang, Feng,Li, Jia,Qu, Bingxue,Xu, Gaoya,Ying, Huazhou,Zhang, Jianjun,Zhang, Mengmeng,Zhou, Yubo
, (2020/07/15)
The enzymes involved in the metabolic pathways in cancer cells have been demonstrated as important therapeutic targets such as the isocitrate dehydrogenase 2 (IDH2). A series of macrocyclic derivatives was designed based on the marketed IDH2 inhibitor AG-221 by using the conformational restriction strategy. The resulted compounds showed moderate to good inhibitory potential against different IDH2-mutant enzymes. Amongst, compound C6 exhibited better IDH2R140Q inhibitory potency than AG-221, and showed excellent activity of 2-hydroxyglutarate (2-HG) suppression in vitro and its mesylate displayed good pharmacokinetic profiles. Moreover, C6 performed strong binding mode to IDH2R140Q after computational docking and dynamic simulation, which may serve as a good starting point for further development.
IMIDAZOPYRAZINE DERIVATIVES AS ANTIBACTERIAL AGENTS
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Page/Page column 44; 315, (2020/07/14)
The invention provides novel imidazopyrazine derivatives having the general formula (I), wherein A and R1 to R11 are as described herein NA (I) and pharmaceutically acceptable salts thereof.5 Further provided are pharmaceutical compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds as medicaments, in particular methods of using the compounds as antibiotics for the treatment or prevention of bacterial infections and resulting diseases.
