Conventional Tetrakis(triphenylphosphine)palladium‐Copper(I) Iodide‐Catalyzed Sonogashira Coupling of Free and BOC‐ Protected Propargylic Amines “On Water”

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Alkynylation of aryl iodides with propargylic amines has been achieved by means of a Sonogashira coupling using “on water” methods. The use of less than 0.2 mol% of tetrakis(triphenylphosphine)palladium [Pd(PPh3)4] and 1.5 mol% copper(I) iodide [CuI] in the presence of diisopropylethylamine (DIPEA) allows the coupling to proceed at 95 °C yielding moderate to good yields of mono‐, bis‐, and tris‐aminoalkynylbenzene derivatives.