99765-13-6Relevant articles and documents
Palladium-catalyzed C-H olefination of uracils and caffeines using molecular oxygen as the sole oxidant
Zhang, Xinyu,Su, Lv,Qiu, Lin,Fan, Zhenwei,Zhang, Xiaofeng,Lin, Shen,Huang, Qiufeng
, p. 3499 - 3506 (2017/04/26)
The palladium-catalyzed oxidative C-H olefination of uracils or caffeines with alkenes using an atmospheric pressure of molecular oxygen as the sole oxidant has been disclosed. This novel strategy offers an efficient and environmentally friendly method to
Copper-catalyzed direct thiolation of xanthines and related heterocycles with disulfides
He, Zuying,Luo, Fang,Li, Yinglong,Zhu, Gangguo
supporting information, p. 5907 - 5910 (2013/10/21)
A novel copper-catalyzed, base-free direct thiolation of xanthines and related heterocycles is described, featuring the use of inexpensive Cu(OAc) 2·H2O as the catalyst, O2 as a clean and cheap oxidant, and easy-to-handle
Dehydrogenative Heck coupling of biologically relevant N-heteroarenes with alkenes: Discovery of fluorescent core frameworks
Huang, Yumin,Song, Feijie,Wang, Zhen,Xi, Peihua,Wu, Ningjie,Wang, Zhigang,Lan, Jingbo,You, Jingsong
supporting information; experimental part, p. 2864 - 2866 (2012/04/17)
A Pd/Cu-catalyzed dehydrogenative Heck coupling is established that allows direct alkenylation of various biologically relevant N-heteroarenes with alkenes. The resulting π-extended alkenylated N-heteroarenes exhibit interesting fluorescent properties and have proven to be potentially useful fluorescent probes for bioimaging. The Royal Society of Chemistry 2012.
Pd/Cu-catalyzed direct alkenylation of azole heterocycles with alkenyl halides
Sahnoun, Sophian,Messaoudi, Samir,Brion, Jean-Daniel,Alami, Mouad
experimental part, p. 6097 - 6102 (2011/02/28)
Direct alkenylation of azole heterocycles through Pd-Cu-catalyzed C-H bond activation has been reported using alkenyl bromides as the coupling partners. The reaction enables the introduction of various mono-, di-, or trisubstituted alkenyl bromides as wel
Inhibition of monoamine oxidase B by analogues of the adenosine A2A receptor antagonist (E)-8-(3-chlorostyryl)caffeine (CSC)
Vlok, Nevil,Malan, Sarel F.,Castagnoli Jr., Neal,Bergh, Jacobus J.,Petzer, Jacobus P.
, p. 3512 - 3521 (2007/10/03)
The adenosine A2A receptor has emerged as a possible target for the treatment of Parkinson's disease (PD). Evidence suggests that antagonism of the A2A receptor not only improves the symptoms of the disease but may also protect again
Inhibition of monoamine oxidase B by selective adenosine A2A receptor antagonists
Petzer, Jacobus P.,Steyn, Salome,Castagnoli, Kay P.,Chen, Jiang-Fan,Schwarzschild, Michael A.,Van Der Schyf, Cornelis J.,Castagnoli, Neal
, p. 1299 - 1310 (2007/10/03)
Adenosine receptor antagonists that are selective for the A2A receptor subtype (A2A antagonists) are under investigation as possible therapeutic agents for the symptomatic treatment of the motor deficits associated with Parkinson's disease (PD). Results of recent studies in the MPTP mouse model of PD suggest that A2A antagonists may possess neuroprotective properties. Since monoamine oxidase B (MAO-B) inhibitors also enhance motor function and reduce MPTP neurotoxicity, we have examined the MAO-B inhibiting properties of several A2A antagonists and structurally related compounds in an effort to determine if inhibition of MAO-B may contribute to the observed neuroprotection. The results of these studies have established that all of the (E)-8-styrylxanthinyl derived A2A antagonists examined display significant MAO-B inhibitory properties in vitro with Ki values in the low μM to nM range. Included in this series is (E)-1,3-diethyl-8-(3,4-dimethoxystyryl)-7-methylxanthine (KW-6002), a potent A2A antagonist and neuroprotective agent that is in clinical trials. The results of these studies suggest that MAO-B inhibition may contribute to the neuroprotective potential of A2A receptor antagonists such as KW-6002 and open the possibility of designing dual targeting drugs that may have enhanced therapeutic potential in the treatment of PD.
Synthesis of 8-substituted xanthine derivatives by Suzuki cross-coupling reaction
Vollmann, Karl,Mueller, Christa E.
, p. 871 - 879 (2007/10/03)
A Suzuki cross-coupling reaction procedure was developed to prepare 8-substituted 3,7-dihydropurine-2,6-dione (xanthine) derivatives. 8-Halogen-substituted xanthines were reacted with phenyl- and styrylboronic acids. The best results were obtained using tetrakis(triphenylphosphine)palladium(0) and tripotassium phosphate in dimethylformamide. The developed procedure allows for a convergent synthesis of pharmacologically active 8-substituted xanthine derivatives.
Structure-activity relationships of 8-styrylxanthines as A2-selective adenosine antagonists
Jacobson,Gallo-Rodriguez,Melman,Fischer,Maillard,Van Bergen,Van Galen,Karton
, p. 1333 - 1342 (2007/10/02)
A series of substituted 8-styryl derivatives of 1,3,7-alkylxanthines was synthesized as potential A2-selective adenosine receptor antagonists, and the potency at rat brain A1- and A2-receptors was studied in radioligand bi
