Method for the preparation of taxol and its derivatives

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 263/16 (2006.01) C07D 263/04 (2006.01) C07D 305/14 (2006.01) C07D 413/12 (2006.01)

Patent

CA 2197467

The invention refers to a process for the preparation of compounds of formula (I), wherein R1 is an aryl or heteroaryl group; R2 is hydrogen, arylcarbonyl, heteroarylcarbonyl or C1-C6 alkoxycarbonyl; R3 is hydrogen or acetyl; the process comprising reacting a compound of formula (II) with a compound of formula (III), wherein each of R8 and R9 independently is a hydroxy protecting group in the presence of a condensing agent so obtaining a compound of formula (IV).

L'invention concerne un procédé de préparation de composés de formule (I), dans laquelle R1 représente un groupe aryle ou hétéroaryle; R2 représente hydrogène, arylcarbonyle, hétéroarylcarbonyle ou alkoxycarbonyle C1-C6; R3 représente hydrogène ou acétyle. Le procédé consiste à faire réagir un composé de formule (II) avec un composé de formule (III), dans laquelle R8 et R9 représentent chacun indépendamment un groupe inhibant hydroxy en présence d'un agent de condensation afin d'obtenir un composé de formule (IV).

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