WO2010010189 Novel Compounds useful for the treatment of Degenerative and Inflammatory Diseases

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Scaffold: Triazolopyridine

Biological target:

Janus kinase: JAK 

Activity:

Inhibitor

Steps Conditions Reactions
a PdCl2dppf, K2CO3, dioxan/water (5/1), microwave irradiations, 140oC Suzuki cross coupling reaction
b NaOH 2N, H2O/MeOH (1/1), 1h30 Saponification
c EDCI, HOBt, DMF, 16h Amide bond formation
d NaNO2, 57% aqueous HI, DMSO, 35oC Sandmeyer reaction
e Pd(OAc)2, BINAP, Cs2CO3, sealed tube, 120oC Buchwald-Hartwig cross coupling reaction

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