C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 305/14 (2006.01) C07D 407/12 (2006.01)
Patent
CA 2307548
A process for the preparation of taxol, analogs thereof and their intermediates is described. The process includes the steps of protecting the C- 7 hydroxy group of 9-dihydro-13-acetylbaccatin III with a suitable protecting group; oxidizing the C-9 hydroxy group; and adding a suitable side chain to the C-13 position. The intermediates include a compound having formula (1) wherein R is selected from the group consisting of benzyl, substituted benzyl, benzylformate, substituted benzylformate, tosyl, substituted tosyl, dihydropyran, methoxymethyl, benzoyl and substituted benzoyl.
L'invention concerne un procédé permettant de préparer du Taxol et des analogues du Taxol, ainsi que leurs intermédiaires. Selon le procédé, on protège le groupe hydroxy en C7 de la 9-dihydro-13-acétylbaccatine III par un groupe protecteur approprié; on oxyde le groupe hydroxy en C9; et on ajoute un chaîne latérale appropriée en position C13. Parmi les intermédiaires, on trouve un composé de formule (1), dans laquelle R est choisi dans le groupe comprenant benzyle, benzyle substitué, benzylformate, benzylformate substitué, tosyle, tosyle substitué, dihydropyrane, méthoxyméthyle, benzoyle et benzoyle substitué.
Heenan Blaikie Llp
Ivax Research Inc.
Liu Jian
LandOfFree
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