79574-71-3Relevant articles and documents
Design, synthesis, and activity of a series of arylpyrid-3-ylmethanones as type i positive allosteric modulators of α7 nicotinic acetylcholine receptors
Hogenkamp, Derk J.,Ford-Hutchinson, Thomas A.,Li, Wen-Yen,Whittemore, Edward R.,Yoshimura, Ryan F.,Tran, Minhtam B.,Johnstone, Timothy B. C.,Bascom, Gavin D.,Rollins, Hannah,Lu, Lena,Gee, Kelvin W.
, p. 8352 - 8365 (2013/12/04)
A series of novel arylpyrid-3-ylmethanones (7a-aa) were designed as modulators of α7 nicotinic acetylcholine receptors (nAChRs). The methanones were found to be type I positive allosteric modulators (PAMs) of human α7 nAChRs expressed in Xenopus ooctyes. Structure-activity relationship (SAR) studies resulted in the identification of compound 7v as a potent and efficacious type I PAM with maximum modulation of a nicotine EC 5 response of 1200% and EC50 = 0.18 μM. Compound 7z was active in reversing the effect of scopolamine in the novel object recognition (NOR) paradigm with a minimum effective ip dose of 1.0 mg/kg (2.7 μmol/kg). This effect was blocked by the selective α7 nAChR antagonist methyllycaconitine (MLA). These compounds are potent type I positive allosteric modulators of α7 nAChRs that may have therapeutic value in restoring impaired sensory gating and cognitive deficits in schizophrenia and Alzheimer's disease.
Convenient Stille carbonylative cross-couplings using molybdenum hexacarbonyl
Lindh, Jonas,Fardost, Ashkan,Almeida, Maria,Nilsson, Peter
experimental part, p. 2470 - 2472 (2010/07/04)
Palladium catalysis was used in Stille-type carbonylative cross-couplings employing Mo(CO)6 as the carbon monoxide source. Robust and convenient transformations were carried out in closed vessels at 100 °C, providing a set of diaryl ketones in good yields. Aryl triflates and bromides were used as coupling partners with aryl stannanes. Inclusion of the Mo(CO)6 destabilizing agent DBU made this protocol operationally simple and suppressed side-product formation.
New Gilman-type lithium cuprate from a copper(II) salt: synthesis and deprotonative cupration of aromatics
Nguyen, Tan Tai,Chevallier, Floris,Jouikov, Viatcheslav,Mongin, Florence
experimental part, p. 6787 - 6790 (2010/04/29)
Deprotonative cupration of aromatics including heterocycles (anisole, 1,4-dimethoxybenzene, thiophene, furan, 2-fluoropyridine, 2-chloropyridine, 2-bromopyridine, and 2,4-dimethoxypyrimidine) was realized in tetrahydrofuran at room temperature using the Gilman-type amido-cuprate (TMP)2CuLi in situ prepared from CuCl2·TMEDA through successive addition of 1 equiv of butyllithium and 2 equiv of LiTMP. The intermediate lithium (hetero)arylcuprates were evidenced by trapping with iodine, allyl bromide, methyl iodide, and benzoyl chlorides, the latter giving the best results. Symmetrical dimers were also prepared from lithium azine and diazine cuprates using nitrobenzene as an oxidative agent.