New three-component reactions of alkynyl trifluoroborates

ORGN 461

Nicos A. Petasis, petasis@usc.edu and Malgorzata Myslinska. Department of Chemistry and Loker Hydrocarbon Research Institute, University of Southern California, Los Angeles, CA 90089-1661
We have recently developed a number of variations of a three-component reaction between amines, carbonyl compounds and organoboron derivatives. Although this process works well with a variety of organoboron compounds, the use of alkynyl boronic acids and boronates was hampered by their facile decomposition. Herein, we report that this type of three-component process takes place readily with potassium alkynyl trifluoroborates, which are air and water stable and can be used effectively in the presence of a Lewis acid catalyst. This method was employed in the synthesis of a variety of functionalized N-substituted propargylic amines as well as several related amino alcohols and heterocycles, such as piperazin-2-ones. Additional related transformations of alkynyl trifluoroborates will also be reported.