Solé Àvila, HelenaPurins, MikusEichenberger, LucasWaser, Jérôme2024-11-202024-11-202024-11-202024-08-1510.1002/anie.202411383https://infoscience.epfl.ch/handle/20.500.14299/242092Enamines are versatile building blocks for the synthesis of biologically active compounds. Nevertheless, only a limited number of strategies have been reported for preparing trisubstituted enamines in a regio-and stereoselective manner. Herein, we report a regiocontrolled 6-endo and 5-exo tethered carboamination of propargylic alcohols for the synthesis of trisubstituted enamines. High regioselectivity was achieved through fine-tuning of the amine protecting group during the Pd-catalyzed carboamination. The introduced trifluoromethylated tether enables further stereoselective functionalizations, such as hydrogenation and fluorination.entext::journal::journal article::research article