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183232-66-8

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A method for parallel solid-phase synthesis of Lodinated analogues of the CB1 receptor inverse agonist rimonabant
A method for the parallel solid-phase synthesis (SPS) of iodinated analogues of Sanofi-Aventis' type 1 cannabinoid (CB1) receptor Inverse agonist rimonabant (acomplia) has been developed. The method allows the synthesis of a range of C3 amide/hydrazide derivatives from a resin-bound C3 ester precursor. The C-Ge linkage to the Hypogel-200 resin Is stable to the diversification conditions but allows ipsoiododegermylative cleavage using Nal/NCS even for the products containing the oxidatively labile hydrazide moiety.
Spivey, Alan C.,Tseng, Chih-Chung,Jones, Teyrnon C.,Kohler, Andrew D.,Ellames, George J.
supporting information; experimental part
p. 4760 - 4763
(2009/12/27)

Structure-activity relationships of pyrazole derivatives as cannabinoid receptor antagonists
As a potent, specific antagonist for the brain cannabinoid receptor (CB1), the biarylpyrazole N-(piperidin-1-yl)-5-(4-chlorophenyl)-1-(2,4- dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide (SR141716A; 1) was the lead compound for initiating studies desi
Lan, Ruoxi,Liu, Qian,Fan, Pusheng,Lin, Sonyuan,Fernando, Susanthi R.,McCallion, Deirdre,Pertwee, Roger,Makriyannis, Alexandras
p. 769 - 776
(2007/10/03)

Preparation of iodine-123 labeled AM251: A potential spect radioligand for the brain cannabinoid CB1 receptor
We report the synthesis and labeling with iodine-123 of N-(piperidin-1-yl)-5-(4-iodophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole -3-carboxamide (AM251). This compound is an anlog of the recently described cannabinoid receptor antagonist, R141716A,
Lan, Ruoxi,Gatley, S. John,Makriyannis, Alexandros
p. 875 - 881
(2007/10/03)

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Chemical Properties

Appearance/Colour :white solid
Melting Point: 195-196℃
Density: 1.65 g/cm³
Solubility:DMSO: >10 mg/mL, soluble
Storage Temp.:Store at RT
Refractive Index: 1.702
PKA: 11.31±0.20(Predicted)
PSA: 50.16000
LogP: 6.21860

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