914299-79-9Relevant articles and documents
Using the competing enantioselective conversion method to assign the absolute configuration of cyclic amines with BODE’s acylation reagents
Dooley, Charles J.,Burtea, Alexander,Mitilian, Christina,Dao, Wendy T.,Qu, Bo,Salzameda, Nicholas T.,Rychnovsky, Scott D.
, p. 10750 - 10759 (2020/10/02)
The competing enantioselective conversion (CEC) method is a quick and reliable means to determine absolute configuration. Previously, Bode’s chiral acylated hydroxamic acids were used to determine the stereochemistry of primary amines, as well as cyclic and acyclic secondary amines. The enantioselective acylation has been evaluated for 4-, 5-, and 6-membered cyclic secondary amines, including medicinally relevant compounds. The limitations of the method were studied through computational analysis and experimental results. Piperidines with substituents at the 2-position did not behave well unless the axial conformer was energetically accessible, which is consistent with the transition state geometries proposed by Bode and Kozlowski. Control experiments were performed to investigate the cause of degrading selectivity under the CEC reaction conditions. The present study expands the scope of the CEC method for secondary amines and provides a better understanding of the reaction profile.
Aminoheteroaryl benzamides as kinase inhibitors
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, (2016/02/15)
The present invention provides a compound of Formula (I) or a salt thereof; and therapeutic uses of these compounds. The present invention further provides pharmaceutical compositions comprising these compounds, and compositions comprising these compounds with a therapeutic co-agent.
Tertiary amine-promoted enone aziridination: Investigations into factors influencing enantioselective induction
Armstrong, Alan,Pullin, Robert D. C.,Jenner, Chloe R.,Foo, Klement,White, Andrew J. P.,Scutt, James N.
, p. 74 - 86 (2014/02/14)
trans-N-Unsubstituted aziridines were synthesised (up to 77% ee) via a chiral tertiary amine-promoted nucleophilic aziridination of a,b-unsaturated ketones utilising in situ generated N-N ylides (aminimines). A wide range of chiral tertiary amines were sy