1398507-08-8Relevant articles and documents
JAK2 JH2 Fluorescence Polarization Assay and Crystal Structures for Complexes with Three Small Molecules
Newton, Ana S.,Deiana, Luca,Puleo, David E.,Cisneros, José A.,Cutrona, Kara J.,Schlessinger, Joseph,Jorgensen, William L.
supporting information, p. 614 - 617 (2017/06/13)
A competitive fluorescence polarization (FP) assay is reported for determining binding affinities of probe molecules with the pseudokinase JAK2 JH2 allosteric site. The syntheses of the fluorescent 5 and 6 used in the assay are reported as well as Kd results for 10 compounds, including JNJ7706621, NVP-BSK805, and filgotinib (GLPG0634). X-ray crystal structures of JAK2 JH2 in complex with NVP-BSK805, filgotinib, and diaminopyrimidine 8 elucidate the binding poses.
PROCESS FOR THE PREPARATION OF ETRAVIRINE AND INTERMEDIATES IN THE SYNTHESIS THEREOF
-
Page/Page column 12, (2013/05/09)
The present invention includes compounds of Formula (1) of the following structure: or salts thereof, wherein X is a halogen or a tosyl group. Processes for preparing the compounds of Formula (1) are disclosed in the patent application. The compounds of Formula I are useful as intermediates for preparation of Etravirine. The present invention is also directed toward processes for preparing Etravirine.