Potassium Phosphate, Tribasic → HCID 66807275, compound

Participants

Reaction Steps

Using analogous reaction conditions and work up as described for the preparation of Example 1A, 8-fluoro-5-(phenylsulfonyl)-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indol-1-one (I-60a: 450 mg, 1.308 mmol) was reacted with 3-iodo-4-methylpyridine (286 mg, 1.308 mmol), 1,4-dioxane (25 mL), copper iodide (25 mg, 0.13 mmol), trans-N,N′-dimethyl-cyclohexyl-1,2-diamine (58.46 mg, 0.392 mmol) and potassium phosphate (693 mg, 3.27 mmol) at 120° C. overnight to afford the crude product. Purification by column chromatography on silica gel (5% methanol in DCM) afforded 60 mg of the product (15% yield).

Provenance & Evidence