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    4-Amino-substituted pyrazolo[1,5-a][1,3,5]triazin-2-amines: a new practical synthesis and biological activity

    Access Status
    Fulltext not available
    Authors
    Lim, Felicia Phei Lin
    Dolzhenko, Anton
    Date
    2014
    Type
    Journal Article
    
    Metadata
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    Citation
    Lim, F.P.L. and Dolzhenko, A. 2014. 4-Amino-substituted pyrazolo[1,5-a][1,3,5]triazin-2-amines: a new practical synthesis and biological activity. Tetrahedron Letters. 55 (49): pp. 6684-6688.
    Source Title
    Tetrahedron Letters
    DOI
    10.1016/j.tetlet.2014.10.057
    ISSN
    0040-4039
    School
    School of Pharmacy
    URI
    http://hdl.handle.net/20.500.11937/46256
    Collection
    • Curtin Research Publications
    Abstract

    The trichloromethyl moiety was successfully employed as a leaving group in nucleophilic substitutions with various amines for the synthesis of 4-amino-substituted pyrazolo[1,5-a][1,3,5]triazin-2-amines. The key precursor for this reaction, 4-trichloromethylpyrazolo[1,5-a][1,3,5]triazin-2-amine, was prepared via the solvent-dependent condensation of 5-guanidino-3-phenylpyrazole with trichloroacetonitrile. In a broad biological activity screening, some of the prepared compounds were identified as CGRP receptor antagonists.

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