WO2010149769 5-Phenyl-[1,2,4]Triazolo[1,5-A]Pyridin-2-yl Carboxamides as JAK Inhibitors

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Scaffold: Triazolopyridine

Biological target:

Janus kinase: JAK 

Activity:

Inhibitor

Steps Conditions Reactions
a CH2Cl2, 16h
b DIEA, EtOH/MeOH (1/1) reflux Cyclization (triazolopyridine formation)
c

1). Et3N, CH3CN

2). NH3, MeOH (if bis-acylated)

N-acylation

d PdCl2dppf, K2CO3, dioxan/water (5/1), microwave irradiations, 140oC, 30 min Suzuki cross coupling reaction
e Oxalyl chloride, cat DMF, CH2Cl2, 2h Acid chloride formation
f Et3N, CH2Cl2, 16h Amide bond formation

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