Wenshan Ren
2008
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Journal
Chinese Journal of Medicinal Chemistry
Abstract
Aim To synthesize the antitumor agent sunitinib malate.Methods Starting from tert-butyl acetoacetate,2-tert-butyl-4-ethyl-3,5-dimethyl-1H-pyrrole-2,4-dicarboxylate was obtained via classic Knorr pyrrole reaction.After facile decarboxylation,Vilsmeier formylation,and hydrolysis of the ethyl ester,5-formyl-2,4-dimethyl-1H-pyrrole-3-carboxylic acid was formed.Sunitinib was obtained by one-pot reaction of this intermediate with N,N-diethylethylenediamine and 5-fluoro-1,3-dihydro-indol-2-one,then salt formation.Results and conclusion The target compound was synthesized and its structure was identified by 1H-NMR,MS,elemental analysis,and the overall yield was 28%.