Abstract
The 2-amino-6-trifluoromethyl-3H-pyrimidin-4-one 1 was propargylated to give two regioisomers 2, 3 in definite proportions. Both regioisomers 2 and 3 were independently reacted with alkyl, aryl or cycloalkyl substituted azides under Sharpless conditions and were obtained exclusively 1,4–disubstituted triazole tagged trifluoromethyl substituted pyrimidine derivatives 4 and 5 respectively. All the final products were evaluated for cytotoxic activity against four cancer cell lines and promising compounds were identified.
Keywords: Alkylation, Propargyl bromide, 3H-pyrimidin-4-one, Regioisomers, Sharpless conditions, Triazoles.
Letters in Drug Design & Discovery
Title:Studies on Synthesis of Novel Triazolalkyl Tagged Trifluoromethyl Substituted Pyrimidine Derivatives and their Evaluation for Cytotoxic Activity
Volume: 10 Issue: 9
Author(s): Punna Nagender, Gannarapu Malla Reddy, Royya Naresh Kumar, Anugu Chandrashekar Reddy, Loka Reddy Velatooru, Rajesh Pamanji, Janapala Venkateswara Rao and Banda Narsaiah
Affiliation:
Keywords: Alkylation, Propargyl bromide, 3H-pyrimidin-4-one, Regioisomers, Sharpless conditions, Triazoles.
Abstract: The 2-amino-6-trifluoromethyl-3H-pyrimidin-4-one 1 was propargylated to give two regioisomers 2, 3 in definite proportions. Both regioisomers 2 and 3 were independently reacted with alkyl, aryl or cycloalkyl substituted azides under Sharpless conditions and were obtained exclusively 1,4–disubstituted triazole tagged trifluoromethyl substituted pyrimidine derivatives 4 and 5 respectively. All the final products were evaluated for cytotoxic activity against four cancer cell lines and promising compounds were identified.
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Nagender Punna, Reddy Malla Gannarapu, Kumar Naresh Royya, Reddy Chandrashekar Anugu, Velatooru Reddy Loka, Pamanji Rajesh, Rao Venkateswara Janapala and Narsaiah Banda, Studies on Synthesis of Novel Triazolalkyl Tagged Trifluoromethyl Substituted Pyrimidine Derivatives and their Evaluation for Cytotoxic Activity, Letters in Drug Design & Discovery 2013; 10 (9) . https://dx.doi.org/10.2174/1570180811310090010
DOI https://dx.doi.org/10.2174/1570180811310090010 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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