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Letters in Drug Design & Discovery

Editor-in-Chief

ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

Studies on Synthesis of Novel Triazolalkyl Tagged Trifluoromethyl Substituted Pyrimidine Derivatives and their Evaluation for Cytotoxic Activity

Author(s): Punna Nagender, Gannarapu Malla Reddy, Royya Naresh Kumar, Anugu Chandrashekar Reddy, Loka Reddy Velatooru, Rajesh Pamanji, Janapala Venkateswara Rao and Banda Narsaiah

Volume 10, Issue 9, 2013

Page: [865 - 871] Pages: 7

DOI: 10.2174/1570180811310090010

Price: $65

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.


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