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US 5,710,280 AGranted
Preparation of fluconazole and pharmaceutically acceptable salts thereof
AssigneeDevelopment Center for Biotechnology
InventorsKae-Shyang Shih, Lie-Rong Chen, Ching-Wei Liu, Chia-Lin J. Wang
Life of this patent
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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.
Claims20
A process for preparing 2-(2,4-difluorophenyl)-1,3-bis-(1H-1,2,4-triazol-1-yl)propan-2-ol, said process comprising
- (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.
2 more elements
Dependencies are inferred from the claim text.