WO2010059555 Propyl hydroxylase inhibitors

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Biological target:

HIF prolyl-hydroxylase

Activity:

Inhibitor

Steps Conditions Reactions
a SOCl2, MeOH reflux, 19h Esterification
b HNO3, H2SO4, 0oC Nitration
c Zn, AcOH Nitro reduction
d

i).Triphosgene, DIEA, CH2Cl2, overnight

ii). NaOH 6N, MeOH, 45oC, 2h
Urea formation, intramolecular cyclization and saponification
e 2-Chloro-1,3-dimethylimidazolinium chloride, Et3N, DMF Amide bond formation

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