WO2010025087 Prolyl hydroxylase inhibitors

WO2010025087.pdf
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Biological target:

HIF prolyl-hydroxylase

Activity:

Inhibitor

Steps Conditions Reactions
a POCl3                   Cyclisation
b NaH / DMA Nucleophilic substitution
c

NaH / diethylmalonate / THF

Cyclisation
d

PyBOP / Et3N / DIEA / DCM

Amide synthesis (PyBOP Coupling)
e

NaOH 1M / THF

Carboxylic acid synthesis (Ester hydrolysis)

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