Processes for the preparation of 1,3-bis(1,2,4-triazol-1-yl)-pro

Details Processes for the preparation of 1,3-bis(1,2,4-triazol-1-yl)-pro Processes for the preparation of 1,3-bis(1,2,4-triazol-1-yl)-pro

1994-03-24

1996-01-16

Gerstl, Robert

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

5482666, C07D40310, C07D40302

Patent

active

054849365

ABSTRACT:
The invention provides a regiospecific process for the preparation of 1,3-bis(1,2,4-triazol-1-yl)-propan-2-ol derivatives comprising reacting an oxirane acid salt or an oxirane, under acidic conditions, with 4H-4-amino-1,2,4-triazole. The process is particularly useful for preparing fluconazole which is useful in the treatment of fungal infections in animals and humans.

REFERENCES:
patent: 4404216 (1983-09-01), Richardson
Keay, J. et al., "Regiospecific synthesis of 1-substituted-1,2,4-triazoles using 4-amino-1,2,4-triazole," Chemical Specialties USA 1991 Symposium*.
Astleford, B. et al., "Synthesis of 1-Alkyl-1,2,4 triazoles: A New One Pot Regiospecific Procedure," J. Org. Chem., vol. 54 (1989), Feb. pp. 731-732.

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