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

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...

Full description

Bibliographic Details
Main Authors: Lim, Felicia Phei Lin, Dolzhenko, Anton
Format: Journal Article
Published: Pergamon 2014
Subjects:
Online Access:http://hdl.handle.net/20.500.11937/46256
_version_ 1848757508656594944
author Lim, Felicia Phei Lin
Dolzhenko, Anton
author_facet Lim, Felicia Phei Lin
Dolzhenko, Anton
author_sort Lim, Felicia Phei Lin
building Curtin Institutional Repository
collection Online Access
description 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.
first_indexed 2025-11-14T09:29:13Z
format Journal Article
id curtin-20.500.11937-46256
institution Curtin University Malaysia
institution_category Local University
last_indexed 2025-11-14T09:29:13Z
publishDate 2014
publisher Pergamon
recordtype eprints
repository_type Digital Repository
spelling curtin-20.500.11937-462562017-09-13T15:05:24Z 4-Amino-substituted pyrazolo[1,5-a][1,3,5]triazin-2-amines: a new practical synthesis and biological activity Lim, Felicia Phei Lin Dolzhenko, Anton Trichloroacetonitrile Aminolysis Triazine Pyrazole Purine analogue 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. 2014 Journal Article http://hdl.handle.net/20.500.11937/46256 10.1016/j.tetlet.2014.10.057 Pergamon restricted
spellingShingle Trichloroacetonitrile
Aminolysis
Triazine
Pyrazole
Purine analogue
Lim, Felicia Phei Lin
Dolzhenko, Anton
4-Amino-substituted pyrazolo[1,5-a][1,3,5]triazin-2-amines: a new practical synthesis and biological activity
title 4-Amino-substituted pyrazolo[1,5-a][1,3,5]triazin-2-amines: a new practical synthesis and biological activity
title_full 4-Amino-substituted pyrazolo[1,5-a][1,3,5]triazin-2-amines: a new practical synthesis and biological activity
title_fullStr 4-Amino-substituted pyrazolo[1,5-a][1,3,5]triazin-2-amines: a new practical synthesis and biological activity
title_full_unstemmed 4-Amino-substituted pyrazolo[1,5-a][1,3,5]triazin-2-amines: a new practical synthesis and biological activity
title_short 4-Amino-substituted pyrazolo[1,5-a][1,3,5]triazin-2-amines: a new practical synthesis and biological activity
title_sort 4-amino-substituted pyrazolo[1,5-a][1,3,5]triazin-2-amines: a new practical synthesis and biological activity
topic Trichloroacetonitrile
Aminolysis
Triazine
Pyrazole
Purine analogue
url http://hdl.handle.net/20.500.11937/46256