34273-01-3Relevant academic research and scientific papers
para-Selective arylation and alkenylation of monosubstituted arenes using thianthreneS-oxide as a transient mediator
Chen, Xiao-Yue,Nie, Xiao-Xue,Wu, Yichen,Wang, Peng
supporting information, p. 5058 - 5061 (2020/05/18)
Using thianthreneS-oxide (TTSO) as a transient mediator,para-arylation and alkenylation of mono-substituted arenes have been demonstratedviaapara-selective thianthrenation/Pd-catalyzed thio-Suzuki-Miyaura coupling sequence under mild conditions. This reaction features a broad substrate scope, and functional group and heterocycle tolerance. The versatility of this approach was further demonstrated by late-stage functionalization of complex bioactive scaffolds, and direct synthesis of some pharmaceuticals, including Tetriprofen, Ibuprofen, Bifonazole, and LJ570.
4,4-Diphenylpiperidine Compounds or Pharmaceutically Acceptable Salts Thereof, Pharmaceutical Compositions and Uses Thereof
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Paragraph 0086; 0088, (2019/12/06)
The invention belongs to the field of medicine and chemical industry and relates to a 4,4-diphenylpiperidine compound or a pharmaceutically acceptable salt thereof, a pharmaceutical composition comprising the same and uses thereof. In particular, the invention relates to a compound of Formula I or a pharmaceutically acceptable salt thereof, and to a pharmaceutical composition comprising the compound or a pharmaceutically acceptable salt thereof. In the present invention, the compound or pharmaceutically acceptable salt thereof and the pharmaceutical composition have significant activity in blocking an N-type calcium channel, and have good pharmacokinetic properties, can effectively relieve pain, and have a potentialas a new medicament for prevention or treatment of pain, stroke, cerebral ischemia, alcohol addiction, alcoholism, kidney disease, addictive disorder caused by analgesic or tolerance disorder caused by analgesic.
Bicyclic Benzimidazole Compounds and Their Use as Metabotropic Glutamate Receptor Potentiators
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Page/Page column 66, (2009/08/14)
Compounds of Formula I: wherein A, B, D, L, R1, R2, R3, R4, m, and n are as defined for Formula I in the description. The invention also relates to processes for the preparation of the compounds and to new intermediates employed in the preparation, pharmaceutical compositions containing the compounds, and to the use of the compounds in therapy.
Pyridine, pyrimidine, quinoline, quinazoline, and naphthalene urotensin-II receptor antagonists
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, (2008/06/13)
The present invention relates to urotensin II receptor antagonists, pharmaceutical compositions containing them and their use.
Synthesis of aryl-substituted piperidines by superacid activation of piperidones
Klumpp, Douglas A.,Garza, Manuel,Jones, Andre,Mendoza, Saray
, p. 6702 - 6705 (2007/10/03)
Diarylpiperidines (8-12) may be prepared in good to excellent yields (80-99%) by the reaction of piperidones (3d-h) with benzene and the Bronsted superacid, trifluoromethanesulfonic acid (CF3-SO3H, TfOH). Tropinone (6) and quinuclidone (7) also react in good yields with benzene in TfOH to give the condensation products (13 and 14). Ketal and acetal derivatives also give condensation products (8 and 24) upon reaction with C6H6 in TfOH. The conversion of 3g to 11 is sensitive to both acid quantity and acid strength; a mechanism is proposed for the conversion that invokes dicationic intermediates.
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.
