Process for the preparation of thalidomide

Details Process for the preparation of thalidomide Process for the preparation of thalidomide

C - Chemistry, Metallurgy

07

D

C07D 401/04 (2006.01) A61K 31/454 (2006.01) C07C 229/34 (2006.01) C07D 209/46 (2006.01) C07D 209/48 (2006.01) C07D 211/88 (2006.01) C07D 213/55 (2006.01) C07D 401/06 (2006.01) C07D 401/12 (2006.01) C07D 403/06 (2006.01) C07D 405/12 (2006.01)

Patent

CA 2166315

A process of preparing thalidomide in which N- phthaloylglutamine or N-phthaloylisoglutamine is cyclized with N,N'-carbonyldiimidazole, characterised in that the process comprises heating said N-phthaloylglutamine or N- phthaloylisoglutamine and N,N'-carbonyldiimidazole in refluxing anhydrous tetrahydrofuran.

Les imides cycliques sont des inhibiteurs du facteur de nécrose tumorale alpha et peuvent être utilisés contre la cachexie, le choc endotoxinique et la réplication de rétrovirus. Le [3-phtalimido-3-(3,4-diméthoxyphényl)]propionate de méthyle en est un exemple typique de mode de réalisation.

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