Patent · US Expired

Preparation of fluconazole and pharmaceutically acceptable salts thereof

US5710280A · kind A · utility

6Cited by
1References
20Claims
0Family size

Assignee

Inventors

Key dates

Filing dateJul 9, 1996
Grant dateJan 20, 1998
Priority date
Expiry dateJul 9, 2016

Classification

  • Technology area (CPC C)Chemistry; Metallurgy
  • CPC primaryC07D249/08
  • WIPO fieldOrganic fine chemistry
  • WIPO sectorChemistry

Abstract

A process for preparing fluconazole, including the steps of (1) acylating 1,3-difluorobenzene (DFB) to obtain 2-chloro-2',4'-difluoroacetophenone (CAP); (2) alkylating 4-amino-4H-1,2,4-triazole (4-AT) with CAP to obtain 2-(1H-1,2,4-triazol-1-yl)-2',4'-difluoroacetophenone (TAAP) salt; (3) deaminating TAAP salt to obtain TAAP; and (4) reacting TAAP with 1,2,4-triazole to obtain fluconazole.

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