182369-73-9

Usage

Uses

Voriconazole

Upstream product

• 30537-73-6 4-ethylpyrimidine 
• 86404-63-9 1-(2,4-difluorophenyl)-2-(1H-1,2,4-triazolyl)ethanone 
• 288-88-0 1,2,4-Triazole 
• 124-63-0 methanesulfonyl chloride 
• 141602-25-7 4-chloro-6-ethylpyrimidine 
• 124703-78-2 6-ethylpyrimidin-4-ol 
• 188416-44-6 3-(4-chloropyrimidin-6-yl)-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)butan-2-ol 
• 109-72-8 n-butyllithium 

Relevant academic research and scientific papers

Synthesis method of voriconazole impurity B

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

Preparation of triazoles by organometallic addition to ketones and intermediates therefor

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.

Novel antifungal 2-aryl-1-(1H-1,2,4-triazol-1-yl)butan-2-ol derivatives with high activity against Aspergillus fumigatus

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.

Triazole antifungal agents

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).