89940-71-6Relevant academic research and scientific papers
Biocatalytic Access to Piperazines from Diamines and Dicarbonyls
Borlinghaus, Niels,Gergel, Sebastian,Nestl, Bettina M.
, p. 3727 - 3732 (2018/04/14)
Given the widespread importance of piperazines as building blocks for the production of pharmaceuticals, an efficient and selective synthesis is highly desirable. Here we show the direct synthesis of piperazines from 1,2-dicarbonyl and 1,2-diamine substrates using the R-selective imine reductase from Myxococcus stipitatus as biocatalyst. Various N- and C-substituted piperazines with high activity and excellent enantioselectivity were obtained under mild reaction conditions reaching up to 8.1 g per liter.
2,2,6- and 2,3,5-trimethylpiperazines as monocyclic analogues of the μ-opioid agonist 3,8-diazabicyclo[3.2.1]octanes: Synthesis, modeling, and activity
Ballabio, Manuela,Barlocco, Daniela,Cignarella, Giorgio,Colombo, Diego,Toma, Lucio
, p. 1481 - 1490 (2007/10/03)
A series of trimethylpiperazine derivatives, struturally related to the μ-agonist 3-cinnamyl-8-propionyl-3,8-diazabicyclo[3.2.1]octane have been synthesized and rested in binding studies, using 3H-DAMGO as μ-selective ligand. Their different affinity towards μ-opioid receptors has been interpreted on the basis of a molecular modeling study performed through molecular mechanics calculations and high field 1H MNR spectroscopy.
Reduction of Heterocycles with Nickel-Aluminum Alloy
Lunn, George
, p. 1043 - 1046 (2007/10/02)
Pyrazines, pyridazines, isoxazoles, oxazole, 4-methylpyrimidine, and indole are reduced by nickel-aluminum alloy in potassium hydroxide solution.The reaction is simple to carry out and does not require special apparatus or hydrogen atmospheres.The products were the fully hydrogenated species although benzene rings were not attacked. 4-Methylpyrimidine gave 1,3-diaminobutane and oxazole gave 2-(methylamino)ethanol.It was found that the reaction frequently exhibited an induction period.
