C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 305/14 (2006.01) A61K 31/337 (2006.01)
Patent
CA 2599888
The present invention relates to a new process for the preparation of 9- dihydrobaccatin III intermediates as useful precursors for the preparation of paclitaxel, 1, docetaxel, 2, and analogues thereof. More particularly, the process comprises the steps of (i) concomitantly deacetylating esters at the 10-position and 13-position of 9-dihydro-13-acetylbaccatin III to form 9- dihydro-10-deacetylbaccatin III; (ii) protecting a hydroxy group at the 7- position of 9-dihydro-10-deacetylbaccatin III; and (iii) acylating a hydroxy group at the 10-position to form a compound of formula II.
La présente invention concerne un nouveau processus de préparation d~intermédiaires de la 9-dihydrobaccatine III en tant que précurseurs utiles pour la préparation de paclitaxel, 1, docétaxel, 2, et analogues de ceux-ci. Plus spécifiquement, le processus décrit dans cette invention comprend les étapes consistant à (i) désacétyler de manière concomitante les esters en position 10 et 13 position de la 9-dihydro-13-acétylbaccatine III, afin de former de la 9-dihydro-10-désacétylbaccatine III; (ii) protéger un groupe hydroxy en position 7 de la 9-dihydro-10-désacétylbaccatine III; et (iii) acyler un groupe hydroxy en position 10- afin de former un composé de formule II.
Caron Gaetan
Lourdusamy Mettilda
Accord Health Care Inc.
Bioxel Pharma Inc.
Moffat & Co.
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