Preparation of terazosin hydrochloride dihydrate

Details Preparation of terazosin hydrochloride dihydrate Preparation of terazosin hydrochloride dihydrate

C - Chemistry, Metallurgy

07

D

C07D 405/14 (2006.01) C07D 405/12 (2006.01)

Patent

CA 2309829

A process for the preparation of 1-(4-amino-6,7-dimethoxy-2-quinazolinyl)-4-(2- tetrahydrofuroyl)piperazine hydrochloride dihydrate, and the product produced thereby, comprising reacting by heating 2-chloro-4-amino-6,7- dimethoxyquinazoline and 1-(2-tetrahydrofuroyl)piperazine in a polar organic reaction solution, wherein the polar organic reaction solution comprises a polar organic solvent and a minimum amount of water effective to produce 1-(4- amino-6,7-dimethoxy-2-quinazolinyl)-4-(2-tetrahydrofuroyl)piperazine hydrochloride dihydrate. The heat is added, preferably at reflux for a period of time, after which the reaction solution is allowed to cool to room temperature and the crystalline product 1-(4-amino-6,7-dimethoxy-2- quinazolinyl)-4-(2-tetrahydrofuroyl)piperazine hydrochloride dihydrate is filtered and dried.

On décrit un procédé de préparation de dihydrate du chlorhydrate de 1-(4-amino-6,7-diméthoxy-2-quinazolinyl)-4-(2-tétrahydrofuroyl)pipérazine, et le produit ainsi obtenu. Le procédé consiste à mettre en réaction par chauffage 2-chloro-4-amino-6,7-diméthoxyquinazoline et 1-(2-tétrahydrofuroyl)pipérazine dans une solution de réaction organique polaire, ladite solution contenant un solvant organique polaire et une quantité minimale d'eau suffisante pour produire le dihydrate du chlorhydrate de 1-(4-amino-6,7-diméthoxy-2-quinazolinyl)-4-(2-tétrahydrofuroyl)pipérazine. La chaleur est ajoutée, de préférence par reflux, pendant un laps de temps donné, après quoi la solution de réaction est refroidie à température ambiante et le produit cristallin dihydrate du chlorhydrate de 1-(4-amino-6,7-diméthoxy-2-quinazolinyl)-4-(2-tétrahydrofuroyl)pipérazine est filtré et séché.

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