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Volumn 21, Issue 6, 2011, Pages 1865-1870

Design of a novel pyrrolidine scaffold utilized in the discovery of potent and selective human β3 adrenergic receptor agonists

Author keywords

3 Adrenergic receptor agonist; Pyrrolidine scaffold

Indexed keywords

BETA 3 ADRENERGIC RECEPTOR; BETA 3 ADRENERGIC RECEPTOR STIMULATING AGENT; CARBON; CL 316423; CYTOCHROME P450 2D6; CYTOCHROME P450 3A4; ETHANOLAMINE; L 796568; MIRABEGRON; NITROGEN; PYRROLIDINE DERIVATIVE; RITOBEGRON; UNCLASSIFIED DRUG;

EID: 79952362760     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2010.12.087     Document Type: Article
Times cited : (9)

References (39)
  • 23
    • 79952360328 scopus 로고    scopus 로고
    • For the purpose of easier synthetic manipulation, the phenyl analog of L-796,568 was chosen for comparison since it has similar in vitro potency and metabolic properties as L-796,568
    • For the purpose of easier synthetic manipulation, the phenyl analog of L-796,568 was chosen for comparison since it has similar in vitro potency and metabolic properties as L-796,568.
  • 28
    • 79952364497 scopus 로고    scopus 로고
    • Zhan Catalyst I is available from Zannan Pharma LTD, catalog number RC-301. Patents CN1907992A, US 2007/0043180 A1, PCT WO 2007/003135 A1
    • Zhan Catalyst I is available from Zannan Pharma LTD, catalog number RC-301. Patents CN1907992A, US 2007/0043180 A1, PCT WO 2007/003135 A1.
  • 29
    • 79952364083 scopus 로고    scopus 로고
    • 10
    • 10
  • 30
    • 79952360625 scopus 로고    scopus 로고
    • The major isomer eluted first at retention time of 4.11 min, while the second isomer eluted at 4.56 min.
    • The major isomer eluted first at retention time of 4.11 min, while the second isomer eluted at 4.56 min.
  • 31
    • 79952361334 scopus 로고    scopus 로고
    • The stereochemistry of the two pyrrolidine chiral centers was determined to be cis based on 2D NOE NMR data (see Supplementary data)
    • The stereochemistry of the two pyrrolidine chiral centers was determined to be cis based on 2D NOE NMR data (see Supplementary data).
  • 32
    • 79952362676 scopus 로고    scopus 로고
    • Selectivity was assessed by SFC analytical analysis and the effort to improve selectivity was studied via trial and error of changes in the reaction conditions. Original less selective conditions: Dilution 0.02 M and stoichiometric amount (by weight) of the catalyst (resulted in 3:1 mixture of cis/trans)
    • Selectivity was assessed by SFC analytical analysis and the effort to improve selectivity was studied via trial and error of changes in the reaction conditions. Original less selective conditions: Dilution 0.02 M and stoichiometric amount (by weight) of the catalyst (resulted in 3:1 mixture of cis/trans).


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.