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Synthetic Communications
An International Journal for Rapid Communication of Synthetic Organic Chemistry
Volume 33, 2003 - Issue 20
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Original Articles

New Synthesis of Thymidylate Synthase Inhibitor Raltitrexed

Associate Professor Sheng-Li Cao Department of Chemistry, Capital Normal University, Beijing, P.R. ChinaCorrespondence[email protected]
,
Rong Wan Department of Chemistry, Tsinghua University, Beijing, P.R. China
&
Yu-Ping Feng Department of Chemistry, Tsinghua University, Beijing, P.R. China
Pages 3519-3526 | Received 28 Feb 2003, Published online: 15 Aug 2006
 
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Abstract

The quinazoline-based inhibitor of thymidylate synthase, Raltitrexed, was synthesized from 2,5-thiophenedicarboxylic acid via mono-coupling with diethyl l -glutamate, modified Curtius reaction, N-methylation, removal of Boc-protecting group, condensation with (bromomethyl)quinazolinone and saponification in 18.2% overall yield.

Acknowledgments

We are grateful to the Natural Science Foundation, the Education Committee of Beijing City, and the Ministry of Education of P. R. China for financial support.

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