120717-48-8Relevant articles and documents
PLASMA KALLIKREIN INHIBITORS
-
Page/Page column 177, (2022/01/05)
The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing one or more disease states that could benefit from inhibition of plasma kallikrein, including hereditary angioedema, uveitis, posterior uveitis, wet age related macular edema, diabetic macular edema, diabetic retinopathy and retinal vein occlusion. The compounds are selective inhibitors of plasma kallikrein.
Syntheses of 5-Alkenylpyrimidines by Organotin Reactions
Sandosham, Jessie,Benneche, Tore,Moeller, Bjoerg,Undheim, Kjell
, p. 455 - 461 (2007/10/02)
5-Stannylpyrimidines can be prepared from the corresponding bromides by lithiation at -95 deg C and quenching with tributylstannyl chloride.The 5-stannyl-pyrimidine is used in Pd-catalyzed coupling reactions with vinyl bromides.The opposite reaction sequence, i.e.Pd-catalyzed coupling between 5-halopyrimidines and vinyltin derivatives, is also described.Alternatively, the 5-vinylpyrimidines have been obtained by dehydrohalogenation with cesium fluoride and by a modified Wittig reaction. 2-Methylthiopyrimidines are transformed into the 2-methoxy derivatives or 2-pyrimidinones using chloramine-T (CAT) in a simple one-pot synthesis.