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

Author:
Lim, Felicia Phei Lin, Dolzhenko, Anton V.
Source:
Tetrahedron letters 2014 v.55 no.49 pp. 6684-6688
ISSN:
0040-4039
Subject:
Lewis bases, amines, antagonists, bioactive properties, chemical reactions, moieties, screening
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.
Agid:
5995561