Abstract

The reductive amination of levulinic and 2‐acetyl benzoic acids with hydrogen and various amines proceeds efficiently in the presence of a homogeneous Ni/triphos‐catalyst. The reaction rate of the overall process is significantly enhanced using 3,3,3‐trifluoroethanol (TFE) as solvent. The optimized synthetic protocol allows for a straightforward access of >20 examples of N‐functionalized pyrrolidinones in high yields (75% and >99%). Upscaling to 10 mmol‐scale is demonstrated and mechanistic in situ studies revealed the presence of alkoxy‐ and hydroxylactams as crucial intermediates.

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