Olverembatinib Chemische Eigenschaften,Einsatz,Produktion Methoden
Beschreibung
GZD-824 is an orally available inhibitor of a broad spectrum of Bcr/Abl tyrosine kinase mutants including T315I (IC
50s = 0.34 and 0.68 nM for wild-type Bcr/Abl and Bcr/Abl
T315I, respectively). It has been shown to suppress the proliferation of Bcr/Abl-positive K562 and Ku812 human chronic myelogenous leukemia cells (IC
50s = 0.2 and 0.13 nM, respectively) and induce tumor regression in mouse xenograft tumor models driven by either wild-type or mutant Bcr/Abl.
Verwenden
GZD824 is a orally bioavailable inhibitor that targets phosphorylated and non-phosphorylated Breakpoint Cluster Region-Abelson (Bcr-Abl) kinases. It is a COVID19-related research product.
Synthese
In a recent patent, the synthesis of olverembatinib began with a Sonogashira coupling reaction of commercially available alkyne 24.1 with pyridinium bromide 24.2 to afford ester 24.3 in 98% yield. The N-Boc group of carbonate 24.3 was cleaved by refluxing in a mixture of MeOH and water to afford pyrazole 24.4 in 91% yield. Finally, potassium tert-butoxide-mediated amide formation with aniline 24.5 afforded olverembatinib (24) in 88% yield.
target
BCR-ABL
Olverembatinib Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
