WO 2010135504: Thiazolopyrimidone Derivatives as PI3 Kinase Inhibitors

Biological target:

Phosphatidylinositol 3-kinases-beta: PI3K-beta

Activity:

Inhibitor

Steps Conditions Reactions
a EtOH overnight
b

KSAc, CH3CN

21 wt % NaOEt, EtOH

 

Nucleophilic substitution

c Acetyl chloride, Pyridine, DMAP, 80oC, 2h N-acylation
d K2CO3, DMF, 90oC, 3h Nucleophilic substitution
e sodium perborate tetrahydrate, K2CO3, H2O/MeOH/THF 1/1/1, 50oC, overnight Thiazolopyrimidone formation

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