WO2010022308 Prolyl hydroxylase inhibitors

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Biological target:

HIF prolyl-hydroxylase

Activity:

Inhibitor

Steps Conditions Reactions
a SOCl2 / MeOH Ester synthesis (Esterification)
b HNO3 / H2SO4 Nitration
c

Zn / AcOH 

Primary amine synthesis (nitro reduction)
d

K2CO3 / thiophosgene / CHCl3 

Thiocyanate synthesis
e

1. 2-amino-5,6-dimethoxypyridine / DMF

2. NaOH 10%                               

Cyclisation / Carboxylic acid synthesis (Ester hydrolysis)
f HATU / DIEA / DMF Amide synthesis (HATU coupling)

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