Intermediate for the synthesis of amlodipine, a process for...

C - Chemistry – Metallurgy – 07 – D

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C07D 209/48 (2006.01) C07D 211/90 (2006.01) C07D 401/12 (2006.01)

Patent

CA 2349013

An intermediate for the synthesis of amlodipine, a process for the preparation thereof and the corresponding use are disclosed. The intermediate is ethyl 3-amino-4-(2-(phthalimido)ethoxy)crotonate and is of formula III (See formula III) The process for the preparation thereof comprises reacting the acetoacetate of formula (See formula IV) with ammonium acetate, and the use thereof is for the preparation of the compound of formula (See formula V) the process being conducted by reacting ethyl 3-amino-4-[2- (phthalimido)ethoxy]crotonate with a benzylidene derivative

L'invention concerne un produit intermédiaire permettant la synthèse d'amlodipine, ainsi que les procédés de préparation et d'utilisation dudit produit intermédiaire. Ce produit intermédiaire est le 3-amino-4-(2-phtalimido)éthoxy)crotonate d'éthyle, représenté par la formule (III). Le procédé de préparation consiste à faire réagir l'acétoacétate de formule (A) avec de l'acétate d'ammonium. Ce produit intermédiaire est utilisé dans la préparation du composé de formule (B), que l'on obtient en faisant réagir le 3-amino-4-[2-(phtalimido)éthoxy]crotonate d'éthyle avec un dérivé du benzylidène.

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