WO2010046273 Pyrimidinyl pyridone inhibitors of JNK

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Scaffold: Pyrimidinyl pyridone

Biological target:

c-Jun N-terminal kinases: JNK1, JNK2

Activity:

Inhibitor

Steps Conditions Reactions
a Methyl propionate / K2CO3 / NMP Cyclisation
b trans-4-aminocyclohexanol / NCS / NMP / H2O 
 Secondary amine synthesis (Nucleophilic substitution)

 


Steps Conditions Reactions
a Et3N / THF Secondary amine synthesis (nucleophilic substitution)
b LiAlH4 / THF Hydroxyl synthesis (ester reduction)
c MnO2 / DCM Aldehyde synthesis 
d THF Alkene synthesis (Wittig reaction)
e DBU / DIEA Cyclisation
f cyclohexylamine / NCS / NMP / H2O Secondary synthesis (nucleophilic substitution)
Steps Conditions Reactions
a THF Alkene synthesis (Wittig reaction)
b DBU / DIEA Cyclisation
c NCS / NMP / H2O Secondary amine synthesis (nucleophilic substitution)