Method for preparation of taxol

Details Method for preparation of taxol Method for preparation of taxol

C - Chemistry, Metallurgy

07

D

260/368, 260/369

C07D 205/08 (2006.01) C07D 233/86 (2006.01) C07D 303/00 (2006.01) C07D 305/14 (2006.01) C07F 7/10 (2006.01)

Patent

CA 2016951

A .beta.-lactam of the formula: (see fig. I) wherein R1 is aryl, substituted aryl, alkyl, alkenyl, or alkynyl; R2 is hydrogen, alkyl, acyl, acetal, ethoxyethyl, or other hydroxyl protecting group; and R3 is aryl, substituted aryl, alkyl, alkenyl, or alkynyl, and process for the preparation of taxol comprising contacting said .beta.-lactam and an alcohol in the presence of an activating agent to provide a taxol intermediate, and converting the intermediate to taxol.

Un bêta-lactame de formule (fig. I), où R1 est un aryle ou un alkyle, alcényle, alcynyle ou aryle avec substitution; R2 est un hydrogène, un groupe alkyle, acyle, acétal, éthoxyéthyle ou un autre groupe protecteur de l'hydroxyle; R3 est un aryle ou un alkyle, alcényle, alcynyle ou aryle avec substitution; méthode de préparation de taxol, consistant à mettre en contact le bêta-lactame et un alcool en présence d'un agent d'activation pour obtenir un intermédiaire de taxol, puis ce dernier par conversion de l'intermédiaire.

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