Synthesis of 2-substituted piperazines via direct α-lithiation
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.
Berkheij, Martin,Van Der Sluis, Lisan,Sewing, Claudia,Den Boer, Dennis J.,Terpstra, Jan Willem,Hiemstra, Henk,Iwema Bakker, Wouter I.,Van Den Hoogenband, Adri,Van Maarseveen, Jan H.
p. 2369 - 2371
(2007/10/03)
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