NOVEL PREPARATION METHOD FOR CITALOPRAM AND ESCITALOPRAM USING CARBONATES

The present invention relates to a method for preparing citalopram and escitalopram, and addition salts using same. In the preparation of citalopram and escitalopram, intermediate compounds are not separately obtained before a cyclization process, and 4-[4-(dimethylamino)-1-(4-fluorophenyl)-1-hydroxy-1-butyl]-3-(hydroxymethyl)benzonitrile represented by chemical formula 3 or (S)-(-)-4-(dimethylamino)-1-(4-fluorophenyl)-1-hydroxy-1-butyl]-3-(hydroxymethyl)-benzonitrile represented by chemical formula 3a is cyclized using carbonate compounds without subsequent treatment processes, such as separation and concentration, of intermediate compounds, thereby preparing citalopram and escitalopram with high purity and high yield. La présente invention concerne un procédé de préparation de citalopram et d'escitalopram, ainsi que des sels d'addition les utilisant. Dans la préparation de citalopram et d'escitalopram, des composés intermédiaires ne sont pas obtenus séparément avant un procédé de cyclisation, et du 4-[4-(diméthylamino)-1-(4-fluorophényl)-1-hydroxy-1-butyl]-3-(hydroxyméthyl)benzonitrile représenté par la formule chimique 3 ou du (S)-(-)-4-(diméthylamino)-1-(4-fluorophényl)-1-hydroxy-1-butyl]-3-(hydroxyméthyl)-benzonitrile représenté par la formule chimique 3a est cyclisé à l'aide de composés carbonates sans traitement ultérieur, comme la séparation et la concentration, de composés intermédiaires, ce qui permet de préparer du citalopram et de l'escitalopram présentant une pureté élevée et un haut rendement. 본 발명은 시탈로프람 및 에스시탈로프람의 제조에 있어서 고리화 반응 공정 이전에 중간체 화합물을 별도 분리 수득하지 않고, 화학식 3으로 표시되는 4-[4-(다이메틸아미노)-1-(4-플루오로페닐)-1-하이드록시-1-부틸]-3-(하이드록시메틸)벤조니트릴 또는 화학식 3a로 표시되는 (S)-(-)-4-(다이메틸아미노)-1-(4-플루오로페닐)-1-하이드록시-1-부틸]-3-(하이드록시메틸)-벤조니트릴을 카보네이트 화합물을 이용하여 중간체 화합물의 분리 농축 등의 후속 처리 과정없이 고리화 반응시켜 고순도 및 고수율의 시탈로프람 및 에스시탈로프람을 제조하고, 이를 이용하여 부가염을 제조하는 방법에 관한 것이다.