Method of preparing amino acid taxane derivatives and...

Details Method of preparing amino acid taxane derivatives and... Method of preparing amino acid taxane derivatives and...

C - Chemistry, Metallurgy

07

D

C07D 305/14 (2006.01)

Patent

CA 2499536

Methods of preparing amino acid-substituted taxanes such as: (see formula 4) using selected blocked amino acids are disclosed. After coupling of the blocked amino acid to the taxane, deprotection is carried out with about an equimolar amount of a secondary amine thus substantially avoiding base-catalyzed hydrolysis of amino acid from the taxane. The preferred amino acid-taxanes are useful as intermediates in the production of polymer conjugated therapeutic compositions or as part of pharmaceutically acceptable formulations.

Cette invention concerne des procédés de préparation de taxanes à substitution d'acide aminé représentés par la figure 1 (4) faisant appel à des acides aminés bloqués sélectionnés. Après le couplage de l'acide aminé bloqué au taxane, une déprotection est effectuée à l'aide d'une quantité environ équimolaire d'une amine secondaire, ce qui permet d'éviter l'hydrolyse catalysée par une base d'acide aminé à partir du taxane. Les acide aminé-taxanes de la présente invention peuvent servir d'intermédiaires dans la production de compositions thérapeutiques conjuguées polymères ou de composants de formulations pharmaceutiquement acceptables.

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