Preparation of cabergoline

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 457/06 (2006.01)

Patent

CA 2602898

A method of preparing cabergoline Form I, comprising forming a solvate including cabergoline and a p-disubstituted benzene of formula (A) or 1,3,5- trimethylbenzene and obtaining cabergoline Form I from the solvate. Another aspect of the present invention provides a method for preparing cabergoline Form I comprising dissolving cabergoline in p-disubstituted benzene or 1,3,5- trimethylbenzene and recovering the cabergoline Form I polymorph, suitably by direct crystallization of Form I or by recovery of a solvate which can be converted to Form I. Another aspect of the present invention provides a novel cabergoline polymorph designated cabergoline Form FB and a method of preparing said polymorph by dissolving or forming a solvate of cabergoline in fluorobenzene and recovering cabergoline Form FB.

L'invention concerne une méthode de préparation de cabergoline de formule (I), qui consiste à former un solvate comprenant le cabergoline et un benzène p-disubstitué de formule (A) ou un 1,3,5- triméthylbenzène, pour obtenir un cabergoline de formule (I) à partir du solvate. Un autre aspect de l'invention concerne une méthode de préparation de cabergoline de formule (I), qui consiste à dissoudrte le cabergoline dans un benzène p-disubstitué ou un 1,3,5- triméthylbenzène, puis à récupérer de manière appropriée le polymorphe du cabergoline de formule (I), par cristallisation directe de la formule (I) ou par récupération d'un solvate pouvant être converti en formule (I). Un autre aspect de l'invention concerne un nouveau polymorphe du cabergoline appelé forme posologique FB du cabergoline, et une méthode de préparation dudit polymorphe par dissolution ou formation d'un solvate de cabergoline dans un fluorobenzène, et récupération de la forme posologique FB du cabergoline.

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