C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 211/90 (2006.01)
Patent
CA 2217849
A process for the preparation of methyl 1,1,N-trimethyl-N-(3,3- diphenyl-propyl)-2-aminoethyl 1,4-dihydro-2,6-dimethyl-4-(3- nitrophenyl)-pyridine-3,5-dicarboxylate (lercanidipine) of formula I comprises reacting an acid halide of 2,6-dimethyl- 5-methoxycarbonyl-4-(3-nitrophenyl)- 1,4-dihydropyridine-3-carboxylic acid with 2,N-dimethyl-N-(3,3- diphenylpropyl)-1-amino-2-propanol in an aprotic solvent. The product can be isolated by industrially applicable crystallization techniques and is obtained in high yield as its anhydrous hydrochloride, a form which possesses high stability and low hygroscopicity.
Procédé de préparation de méthyle 1,1,N-triméthyle-N-(3,3-diphénylpropyle)-2-aminoéthyle 1,4-dihydro-2,6-diméthyle-4-(3-nitrophényle)-pyridine-3,5-dicarboxylate (lercanidipine) de formule I, qui consiste à faire réagir un halogénure d'acide de 2,6-diméthyle-5-méthoxycarbonyle-4-(3-nitrophényle)-1,4-dihydropyridine-3-acide carboxylique avec du 2,N-diméthyle-N-(3,3-diphénylpropyle)-1-amino-2-propanol dans un solvant aprotique. Ledit produit peut être isolé par des techniques de cristallisation applicables industriellement et est obtenu dans une quantité élevée en tant que son hydrochlorure anhydre, une forme qui possède une stabilité élevée et une faible hygroscopicité.
Leonardi Amedeo
Motta Gianni
Borden Ladner Gervais Llp
Recordati Ireland Limited
Recordati S.a. Chemical And Pharmaceutical Company
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