2-Pyridinamine, 5-iodo- → Methyl 2-(4-(4-(6-aminopyridin-3-yl)phenyl)-2-oxabicyclo[2.2.2]octan-1-yl)acetate

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Reaction Steps

The title compound was prepared analogous to Example 4, Step 1 starting from methyl 2-(4-(4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)-2-oxabicyclo[2.2.2]octan-1-yl)acetate (200 mg, 0.52 mmol) and 5-iodopyridin-2-amine (137 mg, 0.62 mmol). The reaction was performed at 80° C. for overnight. After workup and column purification afforded the title compound as off-white solid after drying (133 mg, 58% yield). LC/MS, ESI-MS(+):353.3, RT: 1.12 (Condition E).

Provenance & Evidence