C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 217/26 (2006.01)
Patent
CA 2293705
The process for obtaining quinapril hydrochloride (I) comprises the stages of: a) hydrogenolysis of the benzyl ester of quinapril (II) by treatment in an alcoholic solvent, with concentrated hydrochloric acid or a solution of hydrogen chloride in isopropanol, and hydrogenation; b) removal of the solvent; c) addition of toluene to precipitate the quinapril hydrochloride as a toluene solvate; d) treatment of said solvate with a Class 3 solvent which forms a solvate of quinapril hydrochloride from which it can be removed by drying without degrading; and e) drying of the solvate from step d) to yield quinapril hydrochloride (I), an antihypertensive agent.
L'invention concerne un procédé permettant d'obtenir du chlorhydrate de quinapryl (I) consistant à a) effectuer une hydrogénolyse de l'ester benzylique du quinapryl (II) par traitement dans un solvant alcoolique, avec acide chlorhydrique ou avec un chlorure d'hydrogène dissous dans l'isopropanol, et par hydrogénation; à b) retirer le solvant; à c) ajouter du toluène pour précipiter le quinapryl chlorhydrate comme solvate de toluène; à d) traiter ledit solvate avec un solvant de la classe 3 qui forme un solvate de chlorhydrate de quinapryl à partir duquel on peut l'éliminer par séchage sans le dégrader; et à e) sécher le solvate de l'étape d) pour obtenir (I). Ces solvates sont utiles pour isoler et purifier (I) un agent antihypertenseur.
Bartra Sanmarti Marti
Monsalvatje Llagostera Montserrat
Puig Torres Salvador
Tomas Navarro Jaime
Esteve Quimica S.a.
Ridout & Maybee Llp
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