Patent · US Expired

Crystalline citalopram diol intermediate alkali

US7435838B2 · kind B2 · utility

1Cited by
8References
24Claims
0Family size

Assignee

Inventors

Key dates

Filing dateDec 6, 2004
Grant dateOct 14, 2008
Priority date
Expiry dateJan 26, 2025

Classification

  • Technology area (CPC C)Chemistry; Metallurgy
  • CPC primaryC07C255/53
  • WIPO fieldOrganic fine chemistry
  • WIPO sectorChemistry

Abstract

The present invention relates to the diol intermediate of citalopram useful for treatment of depression, which is the crystal of free base of 3-hydroxylmethyl-4-[1-(4-fluorophenyl)-1-hydroxyl-4-(dimethylamino)]butylbenzonitrile and the method of crystallization thereof. The present invention has disclosed the method to prepare pure citalopram and its purified salts through crystallization of the described base; the optical resolution method of citalopram diol intermediate, the method to prepare S-citalopram and its purified salts by crystals mentioned above. The present invention has also disclosed the method to prepare citalopram and its purified salts, S-citalopram and its purified salts, as well as pharmaceutical formulation thereof obtained. Using methods of the present invention, the quality and yield of the product can be significantly improved, and the production cost of the medicinal material can be reduced.

Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.