Synthesis of phenstatin and prodrugs thereof

Details Synthesis of phenstatin and prodrugs thereof Synthesis of phenstatin and prodrugs thereof

C - Chemistry, Metallurgy

07

C

C07C 49/84 (2006.01) A61K 31/075 (2006.01) A61K 31/09 (2006.01) A61K 31/12 (2006.01) A61K 31/122 (2006.01) A61K 31/66 (2006.01) A61P 35/00 (2006.01) C07C 43/215 (2006.01) C07C 69/017 (2006.01) C07C 217/80 (2006.01) C07F 9/12 (2006.01)

Patent

CA 2314510

A newly discovered antineoplastic compound denominated "phenstatin" is herein described as are synthetic methods for producing phenstatin and the active prodrug thereof. Phenstatin was converted to the sodium phosphate prodrug (3d) by a dibenzylphosphite phosphorylation and subsequent hydrogenolysis sequence 3b3c3d. Phenstatin (3b) was found to be a potent inhibitor of tubulin polymerization and the binding of colchicine to tubulin comparable to combretastatin A-4 (1b).

L'invention concerne un nouveau composé antinéoplasique, ci-après dénommé "phenstatine". L'invention concerne également des méthodes synthétiques permettant de produire de la phenstatine ainsi que le promédicament actif de celle-ci. La phenstatine est convertie en promédicament au phosphate de sodium (3d) par phosphorylation de phosphite de dibenzyle, puis par une séquence d'hydrogénolyse (3b?3c?3d). On a découvert que la phenstatine (3b) est un inhibiteur puissant de la polymérisation de la tubuline, la liaison de la colchicine à la tubuline étant comparable à la combrétastatine A-4 (1b)

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