公开(公告)号：US20020128497A1

公开(公告)日：2002-09-12

申请号：US10096149

申请日：2002-03-06

Applicant: H. Lundbeck A/S

Inventor： Eva Bolzonella ,  Andrea Castellin ,  Andrea Nicole

IPC: C07D307/87

CPC classification number: C07D307/87

Abstract: A method for the manufacture of citalopram characterized in (i) reaction of 1-(4-fluorophenyl)-1-(3-dimethylaminopropyl)-5-halophthalane with an activated magnesium to form the Grignard reagent null3-null1-(4-fluorophenyl)-1,3 dihydro-isobenzofuran-1-ylnullpropylnulldimethylamine 5-magnesium halide followed by (ii) reaction of null3-null1-(4-fluorophenyl)-1,3 dihydro-isobenzofuran-1-ylnullpropyl)dimethylamine 5-magnesium halide with a compound containing a nullCN group bound to a leaving group to form citalopram.

Abstract translation: 一种制备西酞普兰的方法，其特征在于（i）1-（4-氟苯基）-1-（3-二甲基氨基丙基）-5-卤代酞菁与活化镁反应形成格利雅试剂[3- [1-（4 - 氟苯基）-1,3-二氢 - 异苯并呋喃-1-基]丙基]二甲胺5-卤化镁，然后（ⅱ）[3- [1-（4-氟苯基）-1,3-二氢 - 异苯并呋喃-1-基] 吡啶-2-基]丙基）二甲胺5-卤化镁与包含与离去基团结合的-CN基团的化合物形成西酞普兰。