4-Amino-substituted pyrazolo[1,5-a][1,3,5]triazin-2-amines: a new practical synthesis and biological activity
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.
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Tetrahedron Letters
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School
School of Pharmacy
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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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