Author/Authors :
J.M.M. and Berkheij، نويسنده , , Martin and van der Sluis، نويسنده , , Lisan and Sewing، نويسنده , , Claudia and den Boer، نويسنده , , Dennis J. and Terpstra، نويسنده , , Jan Willem and Hiemstra، نويسنده , , Henk and Iwema Bakker، نويسنده , , Wouter I. and van den Hoogenband، نويسنده , , Adri and van Maarseveen، نويسنده , , Jan H.، نويسنده ,
Abstract :
A novel efficient synthetic route towards the pharmaceutically relevant 2-substituted piperazine class is described. The key step involves α-lithiation of N-Boc piperazines, followed by reaction with several electrophiles. To obtain high yields, in some cases transmetallation to copper after the lithiation step is required.
Keywords :
Piperazines , Transmetallation , DMG , DOM , ?-Lithiation