[EN] A METHOD FOR THE PREPARATION OF CITALOPRAM ACID ADDITION SALTS<br/>[FR] PROCEDE DE PREPARATION DE SELS D'ADDITION D'ACIDE DE CITALOPRAM
申请人:JUBILANT ORGANOSYS LTD
公开号:WO2005070914A1
公开(公告)日:2005-08-04
The present invention discloses a simple in situ method for the purification of citalopram acid addition salts without isolating crystalline citalopram base as a solid, wherein citalopram base is treated with metal hydrides in solvent medium followed by acid addition, to remove structurally similar impurities by filtration to get crude citalopram acid addition salts. The resulting citalopram salts are subjected to simple purification to get pharmaceutically acceptable acid addition salts. The said citalopram base is prepared by subjecting 5-cyanophthalane to an eco-friendly and safe C-alkylation reaction with 3,N,N dimethylaminopropyl chloride in the presence of strong base in a mixture of dimethylsulfoxide and toluene.
该发明公开了一种简单的原位方法,用于在不将结晶的西酞普兰碱作为固体分离的情况下纯化西酞普兰酸盐,其中将西酞普兰碱在溶剂介质中与金属氢化物处理,然后进行酸盐加成,通过过滤去除结构相似的杂质以获得粗西酞普兰酸盐。得到的西酞普兰盐经过简单纯化以获得药用可接受的酸盐。所述的西酞普兰碱是通过将5-氰基邻苯二甲酸酐与3,N,N-二甲基氨基丙基氯化物在强碱存在下在二甲基亚砜和甲苯混合物中进行环保安全的C-烷基化反应制备的。