Processes for the preparation of atomoxetine hydrochloride

C - Chemistry – Metallurgy – 07 – C

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C07C 213/06 (2006.01) C07C 213/10 (2006.01) C07C 217/48 (2006.01)

Patent

CA 2617261

The present invention provides improved processes for the preparation of atomoxetine hydrochloride under reaction conditions that improve reaction yields and facilitate commercial synthesis, m particular, the invention is directed to the synthesis of atomoxetine HCl by adding HCl to a mixture of (R)- (-)-tomoxetine (S)-(+)- mandelate with an organic solvent, with or without a base and water. In preferred embodiments, the atomoxetine hydrochloride produced is Form A.

L'invention concerne des procédés pour préparer de l'hydrochlorure d'atomoxétine dans des conditions de réaction qui permettent d'accroître les rendements de la réaction et de faciliter une synthèse commerciale. En particulier, l'invention concerne la synthèse d'hydrochlorure d'atomoxétine. Cette méthode de synthèse consiste à ajouter du HCl à un mélange de (R)-(-)-tomoxétine (S)-(+)-mandélate et d'un solvant organique, avec ou sans base et avec ou sans eau. Dans des modes de réalisation préférés de l'invention, l'hydrochlorure d'atomoxétine produite est la forme A.

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