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Volumn 17, Issue 22, 2007, Pages 6250-6256

Heteroatom-linked indanylpyrazines are corticotropin releasing factor type-1 receptor antagonists

Author keywords

Copper mediated coupling; Corticotropin releasing factor type 1 antagonist; Corticotropin releasing hormone type 1; CRF1; CRH1; Pyrazine

Indexed keywords

COPPER; CORTICOTROPIN RELEASING FACTOR ANTAGONIST; CORTICOTROPIN RELEASING FACTOR RECEPTOR 1; INDANYLPYRAZINE DERIVATIVE; PYRAZINE DERIVATIVE; UNCLASSIFIED DRUG;

EID: 35148891651     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2007.09.008     Document Type: Article
Times cited : (42)

References (30)
  • 16
    • 35148900184 scopus 로고    scopus 로고
    • Verhoest, P. R.; Hoffman, R. L.; Corbett, J. W.; Ennis, M. D.; Frank, K. E.; Fu, J. -M. WO 2003/45924.
  • 17
    • 35148853571 scopus 로고    scopus 로고
    • Fu, J. -M.; Corbett, J. W.; Ennis, M. D.; Hoffman, R. L.; Verhoest, P. R. WO 2003/72107.
  • 18
    • 35148886125 scopus 로고    scopus 로고
    • Corbett, J. W.; Ennis, M. D.; Frank, K. E.; Fu, J. -M.; Hoffman, R. L.; Verhoest, P. R. WO 2003/91225.
  • 19
    • 35148896773 scopus 로고    scopus 로고
    • Corbett, J. W.; Fu, J. -M.; Ennis, M. D.; Frank, K. E.; Hoffman, R. L.; Verhoest, P. R. WO 2004/024719.
  • 22
    • 33748903846 scopus 로고    scopus 로고
    • 2 = ethyl) was prepared following a literature procedure in
    • 2 = ethyl) was prepared following a literature procedure in. Sato N., and Matsuura T. J. Chem Soc., Perkin Trans. 1 19 (1996) 2345
    • (1996) J. Chem Soc., Perkin Trans. 1 , vol.19 , pp. 2345
    • Sato, N.1    Matsuura, T.2
  • 23
    • 35148892192 scopus 로고    scopus 로고
    • note
    • 3 and catalytic CuI resulted in complex mixtures containing low yields (<20%) of the desired coupled products. Slightly improved yields were achieved by substituting bromopyrazine 3a with iodopyrazine 3b.
  • 24
    • 35148865180 scopus 로고    scopus 로고
    • note
    • Catalytic use of N,N-dimethylethylenediamine was found to provide slightly improved yields of product compared to the use of trans-1,2-diaminocyclohexane. Also, cesium carbonate provided improved yields over potassium carbonate.
  • 25
    • 35148872176 scopus 로고    scopus 로고
    • note
    • Yields for the coupling reaction ranged from 20% to 70%.
  • 27
    • 35148851482 scopus 로고    scopus 로고
    • note
    • i values) from the competition experiments were calculated using an iterative nonlinear regression curve-fitting program (Prism; GraphPAD Software, San Diego, CA).
  • 28
    • 35148857585 scopus 로고    scopus 로고
    • note
    • BINAP was used as the ligand for the Buchwald amination providing analog 7b in 17% yield.
  • 29
    • 0000662121 scopus 로고    scopus 로고
    • Pyridinones B-4, B-6, and B-8 were prepared from the appropriate alkyl 2-aminopyridine following the procedure described by
    • Pyridinones B-4, B-6, and B-8 were prepared from the appropriate alkyl 2-aminopyridine following the procedure described by. Constable E.C., et al. Inorg. Chim. Acta 252 (1996) 281
    • (1996) Inorg. Chim. Acta , vol.252 , pp. 281
    • Constable, E.C.1


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.