1608477-75-3Relevant academic research and scientific papers
Copper-catalyzed C5-regioselective C-H sulfonylation of 8-aminoquinoline amides with aryl sulfonyl chlorides
Li, Jun-Ming,Weng, Jiang,Lu, Gui,Chan, Albert S.C.
, p. 2121 - 2124 (2016)
Copper-catalyzed C-H sulfonylation of 8-aminoquinoline scaffolds in the unusual C5 position was developed. The protocol using inexpensive CuI as the catalyst and commercially available aryl sulfonyl chlorides as the sulfonylation reagents, shows broad substrate scope, producing moderate to good yield of sulfone. The developed method was conveniently applied to synthesize a potential fluorinated PET radioligand of 5-HT6 serotoninergic receptor. Moreover, mechanistic studies revealed that the reactions underwent a radical process.
Syntheses, radiolabelings, and in vitro evaluations of fluorinated pet radioligands of 5-HT6 serotoninergic receptors
Colomb, Julie,Becker, Guillaume,Fieux, Sylvain,Zimmer, Luc,Billard, Thierry
, p. 3884 - 3890 (2014/05/20)
The 5-HT6 receptors are potent therapeutic targets for psychiatric and neurological diseases (schizophrenia, Alzheimers disease, etc.). However, with lack of specific radiopharmaceuticals, their pharmacology is still incomplete and their exploration is limited to animal models. In this context, we have designed a fluorinated PET radiotracer, [18F]2FNQ1P, that possesses a high affinity and selectivity for 5-HT6. In vitro PET autoradiographies in rat brain sections with this radiotracer were in accordance with the 5-HT6 distribution pattern.
