Abstract
AbstractA general and versatile alkenylation protocol for the synthesis of vinyl‐azaarylmethylamines has been developed. Enabled by a palladium/NIXANTPHOS catalyst, this protocol provides efficient access to a large variety of N‐heterocycles bearing allylic amines in up to 98% yield. A wide variety of azaarylmethylamines bearing 2‐pyridylmethyl, 4‐pyridylmethyl, 2‐(aminomethyl)quinoline aryl motifs and diverse 5 to 7 membered cyclic amines were well tolerated. A gram scale reaction was also used to demonstrate the scalability. This method can be readily adopted by medicinal chemists to prepare valuable scaffolds that were previously difficult to access.magnified image
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