1,4-Dioxane → [6-(3-Amino-phenyl)-imidazo[1,2-a]pyrazin-8-yl]-(1H-indazol-5-yl)-amine

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Reaction Steps

A mixture of 1.00 eq. of (6-Bromo-imidazo[1,2-a]pyrazin-8-yl)-(1H-indazol-5-yl)-amine, 1.1 eq. of R4-substituted boronic acid, and 0.10 eq. of Pd(PPh3)4, 2.2 eq. of K3PO4 in 4:1 1,4-dioxane:water is heated to 90° C. for 24 hr. The mixture is cooled to RT and partitioned between EtOAc and sat. NaHCO3. The aqueous phase is extracted with EtOAc and combined extracts are dried over Na2SO4. The solvent is removed under reduced pressure and the resulting residue is purified by flash chromatography (EtOAc) to yield (5).

Provenance & Evidence