Semple, Graeme; Santora, Vincent J.; Smith, Jeffrey M.; Covel, Jonathan A.; Hayashi, Rena; Gallardo, Charlemagne; Ibarra, Jason B.; Schultz, Jeffrey A.; Park, Douglas M.; Estrada, Scott A.; Hofilena, Brian J.; Smith, Brian M.; Ren, Albert; Suarez, Marissa; Frazer, John; Edwards, Jeffrey E.; Hart, Ryan; Hauser, Erin K.; Lorea, Jodie; Grottick, Andrew J. published an article in 2012, the title of the article was Identification of biaryl sulfone derivatives as antagonists of the histamine H3 receptor: Discovery of (R)-1-(2-(4′-(3-methoxypropylsulfonyl)biphenyl-4-yl)ethyl)-2-methylpyrrolidine (APD916).Application In Synthesis of Benzyl(4-bromophenyl)sulfane And the article contains the following content:
The design of a new clin. candidate histamine-H3 receptor antagonist for the potential treatment of excessive daytime sleepiness (EDS) is described. Phenethyl-R-2-methylpyrrolidine containing biphenylsulfonamide compounds were modified by replacement of the sulfonamide linkage with a sulfone. One compound from this series, APD916 (I) increased wakefulness in rodents as measured by polysomnog. with a duration of effect consistent with its pharmacokinetic properties. The identification of a suitable salt form of I allowed it to be selected for further development. The experimental process involved the reaction of Benzyl(4-bromophenyl)sulfane(cas: 53136-21-3).Application In Synthesis of Benzyl(4-bromophenyl)sulfane
The Article related to biaryl sulfone derivative preparation histamine h3 antagonist sar, apd916 h3 antagonist wakefulness, Pharmacology: Structure-Activity and other aspects.Application In Synthesis of Benzyl(4-bromophenyl)sulfane
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