Synthetic method for the preparation of the antineoplastic...

Details Synthetic method for the preparation of the antineoplastic... Synthetic method for the preparation of the antineoplastic...

C - Chemistry, Metallurgy

07

H

C07H 17/04 (2006.01) C07H 17/08 (2006.01)

Patent

CA 2343803

A synthetic method for the preparation of the anti-tumor drug Etoposide. In one embodiment, the method includes the direct condensation of 4'-demethyl epipodophylloxin with 2,3-di-O-dichloroacetyl-(4,6-O-ethylidene)-.beta.-D- glucopyranose in the presence of trimethylsilyl trifluoromethane sulfonate (TMSOTf) to yield 4'-demethylepipodophyllotoxin-4-(2,3-di-O-dichloroacetyl-4,6- 0-ethylidene)-.beta.-D-glucopyranoside, followed by conversion of the same to etoposide. Other methods include use of different Lewis acids as catalyst, as well as different substituted glucopyranosides. This method provides enhanced yields over existing synthetic techniques, reduced reaction times and permits more favorable isolation reaction procedures.

Cette invention a trait à une technique de synthèse aux fins de la préparation d'un médicament antitumoral, l'étoposide. Dans un mode de réalisation, la technique consiste à condenser, directement, 4'-déméthyl-épipodophylloxine avec 2,3-di-O-dichloroacétyl-(4,6-O-éthylidène)-.beta.-D-glucopyranose en présence de triméthylsilyl trifluorométhane sulfonate (TMSOTf), afin d'obtenir 4'-glucopyranoside. Cette opération est suivie de la transformation du produit ainsi obtenu en étoposide. D'autres techniques reposent sur l'utilisation de divers acides de Lewis en tant que catalyseurs ainsi que de divers glucopyranosides. Cette technique, qui fait montre d'un rendement supérieur à celui des techniques de synthèse existantes, permet de raccourcir les temps de réaction et d'avoir des processus de réaction d'isolation plus avantageux.

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