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Improvement of Synthetic Pathways to Thalidomide Ester Derivatives

Abstract : Three synthetic approaches to N-substituted Thalidomide prodrugs from (S)-phtaloylglutamic acid, (S)-Boc-glutamic acid or phtaloylglutamic anhydride are described and compared. The most efficient method is a one-pot synthesis which allowed to obtain an ester derivative of Thalidomide with 67 % yield.
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Submitted on : Friday, November 22, 2019 - 11:12:28 AM
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Olivier Lafont, Gaël Mansard, François Estour, Hervé Galons. Improvement of Synthetic Pathways to Thalidomide Ester Derivatives. Heterocycles, The Japan Institute of Heterocyclic Chemistry, 2005, 65 (12), pp.2957. ⟨10.3987/COM-05-10532⟩. ⟨hal-02375828⟩



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