31309-39-4Relevant academic research and scientific papers
3-Fluoropiperidines and N-methyl-3-fluoropiperidinium salts: The persistence of axial fluorine
Sun, Aiming,Lankin, David C.,Hardcastle, Kenneth,Snyder, James P.
, p. 1579 - 1591 (2007/10/03)
It has previously been shown that the fluorine atom in N-protonated 3-fluoropiperidine salts in water strongly prefers the axial orientation in the six-membered ring chairs. In the present work we examine the proposition that the N-methyl salts are equall
Synthesis, physico-chemical properties and pharmacological screening results of budipine and related 1-alkyl-4,4-diphenylpiperidines
Schaefer,Hackmack,Eistetter,Krueger,Menge,Klosa
, p. 233 - 240 (2007/10/02)
1-Alkyl-4,4-diphenylpiperidines are accessible in a simple manner and with attractive yields by regioselective reaction of certain piperidine derivatives, particularly 3-aroyl-4-aryl-4-hydroxypiperidines, which can be varied widely at the nitrogen atom, with benzene under Friedel-Crafts conditions. The physico-chemical parameters, which are important for the transport and the distribution of a drug in a living system, are discussed for the 1-tert-butyl derivative (13) (budipine) (pK(a), partition coefficient P, saturation concentration c(s), surface activity, protein binding). Rapid absorption of this drug in man is indicated by the size of the permeability coefficient P(M) of the passive transport through artificial phospholipid collodium membranes as well as the invasion curves calculated from P(M). According to pharmacological screening tests, most of the compounds of this class show marked antagonistic activity against experimentally generated pathological states in mice (tremorine and reserpine antagonism) which suggest their potential use in the therapy of Parkinson's disease. 13 has been selected for detailed investigations. Structure-activity analyses did not readily demonstrate the presence of a relationship between the type of alkyl substituent at the piperidine nitrogen atom and the pharmacological screening results obtained.
4,4-Diarylpiperidine compositions and use
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, (2008/06/13)
4,4-Diarylpiperidine compounds, preferably 4,4-diphenylpiperidine which are substituted or unsubstituted in the 1-position of the piperidine nucleus, such as 1-(lower alkyl)-4,4-diphenylpiperidines, 1-(lower alkyl)-4-phenyl-4-tolylpiperidines, and their s
4,4-Diarylpiperidines and process of making the same
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, (2008/06/13)
4,4-Diarylpiperidine compounds, preferably 4,4-diphenylpiperidine which are substituted or unsubstituted in the 1-position of the piperidine nucleus, such as 1-(lower alkyl)-4,4-diphenylpiperidines, 1-(lower alkyl)-4-phenyl-4-tolylpiperidines, and their s
