WO2010065384 Inhibitors of phosphoinositide dependent kinase 1 (PDK1)

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Scaffold: Pyridone and pyrimidone

Biological target:

Phosphoinositide dependent kinase 1: PDK1

Activity:

Inhibitor

Steps Conditions Reactions
a EtOH Cyclisation
b NaH / DMF Nucleophilic substitution
c NaOH aq / MeOH Carboxylic acid synthesis (Ester hydrolysis)
Steps Conditions Reactions
a NaH / DMF Ether synthesis (aromatic substitution)
b Boc2O / DIEA / THF Boc protection
c Fe / H2O / NH4Cl / EtOH Primary amine synthesis (Nitro reduction)
d CDI / DMF Urea synthesis
e HCl 4N / Dioxane N-Boc deprotection
Steps Conditions Reactions
a HATU / DIEA / DMA Amide synthesis (HATU coupling)

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