- Synthesis method of voriconazole impurity B
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The invention relates to a synthesis method of a voriconazole impurity B. The synthesis method of the voriconazole impurity B comprises the steps of firstly, dissolving formamidine acetate and sodiumtert-butoxide in methyl alcohol, conducting stirring und
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- Preparation of triazoles by organometallic addition to ketones and intermediates therefor
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A process for the preparation of a compound of the formula: or an acid addition or base salt thereof, wherein R is phenyl optionally substituted by 1 to 3 substituents each independently selected from halo and trifluoromethyl; R1 is C1-C6 alkyl; and “Het” is pyrimidinyl optionally substituted by 1 to 3 substituents each independently selected from C1-C4 alkyl, C1-C4 alkoxy, halo, oxo, benzyl and benzyloxy, comprising reacting a compound of the formula: with a compound of the formula wherein X is chloro, bromo or iodo, the reaction taking place in the presence of zinc; at least one of iodine or a Lewis acid; and an aprotic organic solvent: optionally further reacting the resulting compound with an acid or base to form the corresponding acid addition or base salt thereof.
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- Novel antifungal 2-aryl-1-(1H-1,2,4-triazol-1-yl)butan-2-ol derivatives with high activity against Aspergillus fumigatus
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Replacement of one triazole ring of fluconazole with 4-pyridinyl leads to an increase in activity against Aspergillus fumigatus. Introduction of an α-methyl group has a marked additional beneficial effect. Investigation of pyridinyl and pyrimidinyl analogues resulted in the identification of 30 (UK-109,496), voriconazole) which has excellent potency against a broad range of fungal pathogens including A. fumigatus and Candida krusei.
- Dickinson, Roger P.,Bell, Andrew S.,Hitchcock, Christopher A.,Narayanaswami, Subramaniyan,Ray, Stephen J.,Richardson, Kenneth,Troke, Peter F.
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p. 2031 - 2036
(2007/10/03)
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- Triazole antifungal agents
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The invention provides antifungal agents of the formula: STR1 and their pharmaceutically acceptable salts, wherein R is phenyl optionally substituted by 1 to 3 substituents each independently selected from halo and CF3 ; R1 is C1 -C4 alkyl; R2 is H or C1 -C4 alkyl; and "Het", which is attached to the adjacent carbon atom by a ring carbon atom, is selected from pyridinyl, pyridazinyl, pyrimidinyl, pyrazinyl and triazinyl, "Het" being optionally substituted by C1 -C4 alkyl, C1 -C4 alkoxy, halo, CF3, CN, NO2, NH2, --NH(C1 -C4 alkanoyl) or --NHCO2 (C1 -C4 alkyl).
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