A process for the preparation of zofenopril calcium salt

Details A process for the preparation of zofenopril calcium salt A process for the preparation of zofenopril calcium salt

C - Chemistry, Metallurgy

07

D

C07D 207/16 (2006.01) A61K 31/40 (2006.01) A61P 9/00 (2006.01)

Patent

CA 2339283

A process for the preparation of polymorph A of zofenopril calcium salt in substantially pure form, which comprises: a) reaction of S(-)-3-benzoylthio-2-methylpropanoic acid chloride with cis-4-phenylthio-L- proline in water at pH ranging from 9.0 to 9.5 and recovery of zofenopril in the acidic form; b) salification of acid zofenopril with a potassium salt in alcoholic solution, and recovery of the resulting potassium salt; c) conversion of the potassium salt to the calcium salt by addition of a zofenopril potassium salt aqueous solution to a CaCl2 aqueous solution at a temperature of 70-90 °C with simultaneous seeding to promote the precipitation of polymorph A.

La présente invention concerne l'élaboration du polymorphe A du sel calcique du zofénopril sous une forme sensiblement pure. On commence a) par faire réagir le chlorure d'acide S(-)-3-benzoylthio-2-méthylpropanoïque avec du cis-4-phénylthio-L-proline dans l'eau à un pH compris entre 9,0 et 9,5, et l'on récupère le zofénopril sous forme acide. On réalise ensuite b) une salification du zofénopril acide avec un sel de potassium dans une solution alcoolique et on récupère le sel de potassium résultant. On effectue enfin c) la conversion du sel de potassium en sel de calcium par addition d'une solution aqueuse de sel potassique de zofénopril à une solution aqueuse de CaCl2 à une température de 70-90 DEG C avec ensemencement simultané de façon à favoriser la précipitation du polymorphe A.

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