Beta-lactams useful in preparation of taxols

Details Beta-lactams useful in preparation of taxols Beta-lactams useful in preparation of taxols

C - Chemistry, Metallurgy

07

D

C07D 205/08 (2006.01)

Patent

CA 2214051

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.

Bêta-lactame de formule, (voir fig. I) où R1 est un groupe aryle, aryle substitué, alkyle, alkényle ou alkynyle; R2 est un hydrogène, un groupe alkyle, acyle, acétal, éthoxyéthyle ou un autre groupe protecteur hydroxyle, et R3 est un groupe aryle, aryle substitué, alkyle, alkényle ou alkynyle, et procédé pour la préparation de taxol comprenant la mise en contact de ladite bêta-lactame et d'un alcool en présence d'un agent d'activation pour obtenir un intermédiaire du taxol, et la conversion de l'intermédiaire en taxol.

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