Method for producing citalopram salt, a crystalline base of citalopram and pharmaceutical composition comprising the same

摘要

Crystalline citalopram base as well as citalopram hydrochloride and hydrobromide with a purity above 99.8% (wt./wt.), especially above 99.9% (wt./wt.) are new. Independent claims are also included for: (A) the production of a citalopram salt comprising: (a) liberation of citalopram base and precipitation of the liberated base in crystalline form; (b) optional recrystallisation of the crystalline base; and (c) conversion of the crystalline base into a salt; and (B) the production of citalopram base or a citalopram salt comprising (i) removal of one or more impurities of formula (I) from a crude citalopram mixture or a crude citalopram salt by precipitation of crystalline citalopram base; and (ii) optional recrystallisation and/or conversion into a salt. [Image] Z : halo; -O-SO 2-(CF 2) n-CF 3; -CHO; -NHR 1>; -COOR 2>; or -CONR 2>R 3>; n : 0-8; R 1>H or alkylcarbonyl; R 2>and R 3>H; alkyl; optionally substituted aryl; or aralkyl. ACTIVITY : Antidepressant. MECHANISM OF ACTION : Serotonin re-uptake inhibitor.