An improved process for the preparation of temozolomide and...

C - Chemistry – Metallurgy – 07 – D

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C07D 487/04 (2006.01) A61K 31/4188 (2006.01) A61P 35/00 (2006.01) C07D 233/90 (2006.01)

Patent

CA 2664052

A process for the preparation of compounds of formula (IA), where R=CH3 (i.e. temozolomide) comprising diazotizing a compound of the formula (IIA) where in R is as defined above in the presence of at least one metal halide, an acid and a source of nitrous acid, followed by conversion of acidic solution containing temozolomide. The conversion can be carried out by a liquid-liquid extraction technique in a water immiscible solvent. The temozolomide may be further purified in an acetone-water mixture.

Procédé pour la préparation de composés de formule (IA), où R = CH3 (c'est-à-dire du témozolomide), consistant à diazoter un composé de formule (IIA), où R est tel que défini ci-dessus, en présence d'au moins un halogénure de métal, d'un acide et d'une source d'acide nitreux, puis à convertir la solution acide contenant le témozolomide. La conversion peut être effectuée par une technique d'extraction liquide-liquide dans un solvant non miscible avec l'eau. Le témozolomide peut être encore purifié dans un mélange acétone-eau.

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