New process for preparing taxane derivatives; new...

Details New process for preparing taxane derivatives; new... New process for preparing taxane derivatives; new...

Category

C - Chemistry, Metallurgy

Subcategory

07

Subsubcategory

D

IPC codes

C07D 409/12 (2006.01) A61K 31/33 (2006.01) C07D 407/00 (2006.01) C07D 407/12 (2006.01) C07D 409/14 (2006.01) C07D 413/00 (2006.01) C07D 417/00 (2006.01)

Type

Patent

Patent number

CA 2149758

Description

Novel method for the preparation of taxane derivatives having the general formula (I) and pharmaceutical compositions which contain the novel derivatives thus obtained. In the general formula (I), R is hydrogen or acetyl, R1 is benzoyl or R2-O-CO wherein R2 is alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, phenyl or hetérocyclyl and Het is a 5-membered optionally substituted aromatic heterocycle (thiophene, tiazole, furan, pyrrole, imidazole, oxazole, isoxazole, pyrazole). The novel products of formula (I) have remarquable antitumor and antileukemia properties.

2149758 9412484 Nouveau procédé de préparation de dérivés du taxane de formule générale (I) et les compositions pharmaceutiques qui contiennent les nouveaux dérivés ainsi obtenus. Dans la formule générale (I), R représente hydrogène ou acétyle, R1 représente benzoyle ou R2-O-CO dans lequel R2 représente alcoyle, alcényle, alcynyle, cycloalcoyle, cycloalcényle, bicycloalcoyle, phényle ou hétérocyclyle et Het représente un hétérocycle aromatique à 5 chaînons (thiophène, thiazole, furanne, pyrrole, imidazole, oxazole, isoxazole, pyrazole) éventuellement substitué. Les nouveaux produits de formule (I) présentent des propriétés antitumorales et antileucémiques remarquables.

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