New synthesis of thymidylate synthase inhibitor raltitrexed
SL Cao, R Wan, YP Feng
Index: Cao, Sheng-Li; Wan, Rong; Feng, Yu-Ping Synthetic Communications, 2003 , vol. 33, # 20 p. 3519 - 3526
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Citation Number: 7
Abstract
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.
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