(2-Methoxypyridin-4-yl)boronic acid → 4-[5-(2-Methoxy-pyridin-4-yl)-[1,2,4]triazolo[1,5-a]pyrazin-8-ylamino]-N-pyridin-3-ylmethyl-benzamide

Participants

Reaction Steps

This compound may be prepared using methods as described for Compound 6, step 4 using 4-(5-bromo-[1,2,4]triazolo[1,5-a]pyrazin-8-ylamino)-N-pyridin-3-ylmethyl-benzamide (120 mg, 0.28 mmol), 2-methoxypyridine-4-boronic acid (87 mg, 0.57 mmol) and Pd(PPh3)4 (81 mg, 0.07 mmol) in 1.5M K2CO3 (aq) (1.6 mL) and dioxane (2.9 mL). The crude material is purified by silica gel column chromatography eluting with DCM followed by 99:1 then 97:3 then 95:5 DCM:NH3 (7M in MeOH) to afford the title compound as a white solid (92.6 mg, 73%).

Provenance & Evidence