Process of producing amorolfine

Details Process of producing amorolfine Process of producing amorolfine

C - Chemistry, Metallurgy

07

D

C07D 295/03 (2006.01)

Patent

CA 2672404

The present invention refers to an improved process of producing Amorolfine base, which is a compound of formula (I) said process comprising the steps of : (i) contacting a compound of formula (II) with a Friedel-Crafts catalyst; and (ii) adding one equivalent of 2-halogeno-2- methylbutane, characterised in that the reaction mixture obtained in step (i) is cooled to a temperature between -40 to -60 °C prior to step (ii) and the Friedel-Craft catalyst is chosen among the group consisting of gallium chloride, antimony pentafluoride, molybdenum pentachloride, indium chloride, antimony pentachloride.

La présente invention concerne un procédé amélioré de production d'amorolfine base, qui est un composé représenté par la formule (I), ledit procédé comprenant les étapes consistant à : (i) mettre un composé représenté par la formule (II) en contact avec un catalyseur de Friedel-Crafts ; et (ii) ajouter un équivalent de 2-halogéno-2- méthylbutane, caractérisé en ce que le mélange réactionnel obtenu à l'étape (i) est refroidi à une température comprise entre -40 et -60 °C avant l'étape (ii) et en ce que le catalyseur de Friedel-Crafts est choisi parmi le groupe constitué de chlorure de gallium, pentafluorure d'antimoine, pentachlorure de molybdène, chlorure d'indium et pentachlorure d'antimoine.

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