207690-56-0Relevant academic research and scientific papers
Efficient one-pot synthesis of enantiomerically pure: N -protected-α-substituted piperazines from readily available α-amino acids
Jida, Mouhamad,Ballet, Steven
, p. 1595 - 1599 (2018/02/09)
A new pathway towards enantiomerically pure 3-substituted piperazines, bearing a benzyl protecting group, has been developed in good overall yields (83-92%), starting from commercially available N-protected amino acids. The methodology represents an efficient and simple one-pot procedure, employing a synthetic sequence consisting of an Ugi-4 component reaction, a Boc-deprotection, an intramolecular cyclisation reaction and a final reduction (UDCR). From the benzyl protected precursors, the 2-substituted piperazines bearing a Boc-protecting group could consequently also be obtained via a simple protection and deprotection step of the corresponding piperazines. The practical utility of this methodology was demonstrated for chiral drug synthesis.
The Use of Heterocycles for the Conformational Restriction of Biologically Active Peptoids
Horwell, David C.,Lewthwaite, Russell A.,Pritchard, Martyn C.,Ratcliffe, Giles S.,Rubin, J. Ronald
, p. 4591 - 4606 (2007/10/03)
A series of piperazinone ring systems have been synthesized as a means of evaluating the effect of conformational restriction of high affinity non-peptide NK1, NK3 and CCK-B receptor ligands.The synthesis of the targeted heterocycles is described along with a discussion of their affinities for their respective receptor types.
