100858-33-1Relevant articles and documents
NOVEL HETEROCYCLIC COMPOUNDS AS TYROSINE KINASE BCR-ABL INHIBITORS
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Page/Page column 43; 44, (2017/12/09)
Disclosed is a compound of Formula (Ⅰ) or a pharmaceutically acceptable salt thereof, wherein the variables are described herein. Also disclosed is a process for the preparation of compounds, their pharmaceutical compositions comprising the same as an active ingredient, methods using said compositions in the treatment of various disorders, and use of the compounds in the manufacture of a medicament in inhibition of the enzymatic activities of ABL1, ABL2 and related chimeric proteins.
Ultrafast chiral separations for high throughput enantiopurity analysis
Barhate, Chandan L.,Joyce, Leo A.,Makarov, Alexey A.,Zawatzky, Kerstin,Bernardoni, Frank,Schafer, Wes A.,Armstrong, Daniel W.,Welch, Christopher J.,Regalado, Erik L.
supporting information, p. 509 - 512 (2017/01/13)
Recent developments in fast chromatographic enantioseparations now make high throughput analysis of enantiopurity on the order of a few seconds achievable. Nevertheless, routine chromatographic determinations of enantiopurity to support stereochemical investigations in pharmaceutical research and development, synthetic chemistry and bioanalysis are still typically performed on the 5-20 min timescale, with many practitioners believing that sub-minute enantioseparations are not representative of the molecules encountered in day to day research. In this study we develop ultrafast chromatographic enantioseparations for a variety of pharmaceutically-related drugs and intermediates, showing that sub-minute resolutions are now possible in the vast majority of cases by both supercritical fluid chromatography (SFC) and reversed phase liquid chromatography (RP-LC). Examples are provided illustrating how such methods can be routinely developed and used for ultrafast high throughput analysis to support enantioselective synthesis investigations.
An efficient dynamic kinetic resolution of N-heterocyclic 1,2-amino alcohols
Lihammar, Richard,Millet, Renaud,Baeckvall, Jan-E.
supporting information; scheme or table, p. 2321 - 2327 (2011/10/19)
A chemoenzymatic dynamic kinetic resolution (DKR) of N-heterocyclic amino alcohols is described. Various lipases were studied as biocatalysts for the kinetic resolution of N-heterocyclic 1,2-amino alcohols. The influence of the support of the enzymes on t