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Volumn 4, Issue 5, 2002, Pages 442-456

Standardization protocols and optimized precursor sets for the efficient application of automated parallel synthesis to lead optimization: A mitsunobu example

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ARTICLE;

EID: 0037617581     PISSN: 15204766     EISSN: None     Source Type: Journal    
DOI: 10.1021/cc010090j     Document Type: Article
Times cited : (33)

References (36)
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    • Guidelines for drug and analog design
    • Wolf, M. E., Ed.; Wiley-Interscience: New York
    • (a) Craig, P. N. Guidelines for drug and analog design. In The Basis of Medicinal Chemistry; Wolf, M. E., Ed.; Wiley-Interscience: New York, 1980; p 331.
    • (1980) The Basis of Medicinal Chemistry , pp. 331
    • Craig, P.N.1
  • 6
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    • Features and problems in practical drug design
    • Charton, M., Motoc, I., Eds.; Lange and Springer: Berlin
    • (b) Austel, V. Features and problems in practical drug design. In Steric Effects in Drug Design; Charton, M., Motoc, I., Eds.; Lange and Springer: Berlin, 1984; p 8.
    • (1984) Steric Effects in Drug Design , pp. 8
    • Austel, V.1
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    • Experimental design
    • Methods and Principles in Medicinal Chemistry; van de Waterbeemd, H., Ed.; VCH: Weinheim, Germany
    • Austel, V. Experimental design. In Methods and Principles in Medicinal Chemistry; van de Waterbeemd, H., Ed.; Chemometric Methods in Molecular Design, Vol. 2; VCH: Weinheim, Germany, 1995; p 49.
    • (1995) Chemometric Methods in Molecular Design , vol.2 , pp. 49
    • Austel, V.1
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    • Haag, B. T. Chimia 2000, 54, 163.
    • (2000) Chimia , vol.54 , pp. 163
    • Haag, B.T.1
  • 21
    • 0041078035 scopus 로고    scopus 로고
    • PE Biosystems (Applied Biosystems) Solaris 530 organic synthesizer. For additional information see the following
    • PE Biosystems (Applied Biosystems) Solaris 530 organic synthesizer. For additional information see the following: www.appliedbiosystems.com.
  • 24
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    • Wiley: New York
    • (a) Hughes, D. L. Organic Reactions; Wiley: New York, 1992; Vol. 42, p 335.
    • (1992) Organic Reactions , vol.42 , pp. 335
    • Hughes, D.L.1
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    • note
    • 21
  • 28
    • 0041078034 scopus 로고    scopus 로고
    • note
    • 3 {lot number 113-81, loading 1.24 mmol/g}: the percentage of phosphine oxide increased from 23% to 36% over 7 days, atmospheric exposure.
  • 29
    • 0041078037 scopus 로고    scopus 로고
    • note
    • 4 as an external standard. The pulse delay employed was 15 s, and chemical shifts are quoted in ppm. Under these conditions, the phosphine resonance was observed at -6.25 ppm, with the oxide being observed at 29.40 ppm.


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