1. School of Pharmacy, Ohu University, 31-1 Misumido, Tomita-machi, Koriyama, Fukushima 963-8611, Japan;2. Department of Medicinal Chemistry, Hokkaido University of Science, 15-4-1, Maeda 7-jo, Teine-ku, Sapporo, Hokkaido 006-8585, Japan
Abstract:
A method for the catalytic hydrophosphinylation of internal ynamides with H-phosphinates has been developed for the first time. The protocol employing the catalyst generated from NiBr2 and PPh3 could be applied to several types of ynamides and H-phosphinates, affording (E)-β-aminovinylphosphinates in a highly regio- and stereoselective manner.