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Volumn 25, Issue 9, 2015, Pages 1884-1891

Substituted pyrrolidin-2-ones: Centrally acting orexin receptor antagonists promoting sleep. Part 2

Author keywords

CNS drug discovery; Dual orexin receptor antagonists; Metabolic stability; Orexin receptors; Selective orexin 2 receptor antagonists; Sleep

Indexed keywords

2 PYRROLIDONE DERIVATIVE; LACTAM; OREXIN RECEPTOR; OREXIN RECEPTOR ANTAGONIST;

EID: 84930928397     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2015.03.035     Document Type: Article
Times cited : (29)

References (48)
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    • The relative cis-configuration at the two stereogenic centers of 10 was unequivocally established by NOESY experiments. NOEs are observed from the proton of the CH(OH) group to the proton of the CH(aryl) moiety, indicating that the protons H-3 and H-5 are located at the same side of the five-membered ring. For diastereoselective reductions of related 5-arylpyrrolidine-2,3-diones, see
    • The relative cis-configuration at the two stereogenic centers of 10 was unequivocally established by NOESY experiments. NOEs are observed from the proton of the CH(OH) group to the proton of the CH(aryl) moiety, indicating that the protons H-3 and H-5 are located at the same side of the five-membered ring. For diastereoselective reductions of related 5-arylpyrrolidine-2,3-diones, see: P. Camps, T. Gomez, D. Munoz-Torrero, J. Rull, L. Sanchez, F. Boschi, M. Comes-Franchini, A. Ricci, T. Calvet, M. Font-Bardia, E. De Clercq, and L. Naesens J. Org. Chem. 73 2008 6657
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    • DAST-mediated stereocontrolled fluorodehydroxylations of 3-hydroxypyrrolidin-2-ones are known to occur with inversion of stereochemistry: A.G. Avent, A.N. Bowler, P.M. Doyle, C.M. Marchand, and D.W. Young Tetrahedron Lett. 33 1992 1509
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    • A-to-B)] below 3.0 means low affinity of the compound for the human P-gp transporter system.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.