185030-08-4Relevant academic research and scientific papers
Discovery of a Novel Muscarinic Receptor PET Radioligand with Rapid Kinetics in the Monkey Brain
Malmquist, Jonas,Varn?s, Katarina,Svedberg, Marie,Vallée, Frédéric,Albert, Jeffrey S.,Finnema, Sjoerd J.,Schou, Magnus
, p. 224 - 229 (2018/03/01)
Positron emission tomography (PET), together with a suitable radioligand, is one of the more prominent methods for measuring changes in synaptic neurotransmitter concentrations in vivo. The radioligand of choice for such measurements on the cholinergic sy
Stereoselective synthesis of the optical isomers of a new muscarinic receptor antagonist, HL-031120
Liu, Yu-Min,Liu, He,Zhong, Bo-Hua,Liu, Ke-Liang
, p. 1815 - 1822 (2007/10/03)
We present here a practical stereoselective synthetic method to produce enantiopure isomers of a new muscarinic receptor antagonist, HL-031120 (3-quinuclidinyl-2′-cyclopentyl-2′-hydroxy-2′-phenylacetate, I). Four optical isomers were effectively by stereoselective synthesized using pivaldehyde as steric hindrance agent from the chiral starting material, ( S ) or ( R )-mandelic acid. The isomers were obtained with 70-76% yields in 98-99% e.e. Copyright Taylor & Francis Group, LLC.
Stereoselective synthesis of the optical isomers of a new muscarinic receptor antagonist, quinuclidin-3-yl 2-(cyclopent-1-enyl)-2-hydroxy-2- phenylacetate
Liu, Yu-Min,Liu, He,Zhong, Bo-Hua,Liu, Ke-Liang
, p. 335 - 337 (2007/10/03)
The enantiopure isomers of a new muscarinic receptor antagonist, quinuclidin-3-yl 2-(cyclopent-1-enyl)-2-hydroxy-2-phenylacetate were synthesised by a practical stereoselective synthetic method, using pivaldehyde as steric hindrance agent from the chiral starting material, (S) or (R)-mandelic acid. The isomers were obtained with 72-78% yields in 98-99% e.e.
Stereoselective synthesis of 3-azabicyclo[3,3,1]nonan-9α-yl α-(cyclopentyl-1-ene)-α-hydroxy-α-phenylacetate hydrochloride
Liu, He,Han, Xiang-Yu,Zhong, Bo-Hua,Liu, Ke-Liang
, p. 322 - 323 (2007/10/03)
The isomers of α-(cyclopentyl-1-ene)-α-hydroxy-α- phenylacetic acid esters derived from 3-azabicyclo[3,3,1]nonan-9α-ol ((R)-1 and (S)-1) were obtained in high enantiomeric excess by effective stereoselective synthesis from the chiral starting material, (S
1,4-di-substituted piperidine derivatives
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, (2008/06/13)
This invention provides novel 1,4-di-substituted piperidine derivatives of the general formula ?I! STR1 and the pharmaceutically acceptable salts thereof, wherein: Ar represents a phenyl group or a five- or six-membered heteroaromatic group having one or two hetero atoms selected from the group consisting of an oxygen atom, a sulfur atom and a nitrogen atom in which one or two optional hydrogen atoms on the ring may be replaced by substituent groups selected from the group consisting of a halogen atom and a lower alkyl group; R1 represents a cycloalkyl group of 3 to 6 carbon atoms or a cycloalkenyl group of 3 to 6 carbon atoms; R2 represents a saturated or unsaturated aliphatic hydrocarbon radical of 5 to 15 carbon atoms; and X represents O or NH. These compounds have selective antagonistic activity against the muscarinic M3 receptors and can hence be used safely with a minimum of side effects.
