A Novel Series of 4-Piperidinopyridine and 4-Piperidinopyrimidine Inhibitors of 2,3-Oxidosqualene Cyclase-Lanosterol Synthase was written by Brown, George R.;Hollinshead, David M.;Stokes, Elaine S. E.;Waterson, David;Clarke, David S.;Foubister, Alan J.;Glossop, Steven C.;McTaggart, Fergus;Mirrlees, Donald J.;Smith, Graham J.;Wood, Robin. And the article was included in Journal of Medicinal Chemistry in 2000.Quality Control of tert-Butyl 4-(piperidine-4-carbonyl)piperazine-1-carboxylate This article mentions the following:
A novel series of 4-piperidinopyridines and 4-piperidinopyrimidines showed potent and selective inhibition of rat 2,3-oxidosqualene cyclase-lanosterol synthase (OSC) (e.g. 26 IC50 rat = 398±25 nM, human = 112±25 nM) and gave selective oral inhibition of rat cholesterol biosynthesis (26 ED80 = 1.2±0.3 mg/kg, n = 5; HMG-CoA reductase inhibitor simvastatin ED80 = 1.2±0.3 mg/kg, n = 5). The piperidinopyrimidine OSC inhibitors have a significantly lower pKa than the corresponding pyridine or the previously reported quinuclidine OSC inhibitor series. This indicates that other novel OSC inhibitors may be found in analogs of this series across a broader pKa range (6.0-9.0). These series may yield novel hypocholesterolemic agents for the treatment of cardiovascular disease. In the experiment, the researchers used many compounds, for example, tert-Butyl 4-(piperidine-4-carbonyl)piperazine-1-carboxylate (cas: 203520-03-0Quality Control of tert-Butyl 4-(piperidine-4-carbonyl)piperazine-1-carboxylate).
tert-Butyl 4-(piperidine-4-carbonyl)piperazine-1-carboxylate (cas: 203520-03-0) belongs to piperazine derivatives. Piperazine causes primary dermal irritation and skin burns at high concentrations. Piperazine also causes eye irritation in humans. Two common salts in the form of which piperazine is usually prepared for pharmaceutical or veterinary purposes are the citrate, 3C4H10N2.2C6H8O7 (i.e. containing 3 molecules of piperazine to 2 molecules of citric acid), and the adipate, C4H10N2.C6H10O4 (containing 1 molecule each of piperazine and adipic acid).Quality Control of tert-Butyl 4-(piperidine-4-carbonyl)piperazine-1-carboxylate
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics