351227-63-9

Upstream product

• 182760-06-1 ravuconazole 
• 229625-50-7 di-tert-butyl chloromethyl phosphate 

Downstream Products

• 914361-44-7 C₆H₁₄N₂O₂*C₂₃H₂₀F₂N₅O₅PS 
• 942415-34-1 C₂₇H₃₀F₂N₅O₆PS 
• 351227-64-0 4-[2-[(1R,2R)-2-(2,4-difluorophenyl)-1-methyl-2-[(phosphonooxy)methoxy]-3-(1H-1,2,4-triazol-1-yl)propyl]-4-thiazol]benzonitrile 
• 914361-45-8 lysine [{(1R,2R)-2-[4-(4-cyanophenyl)-1,3-thiazol-2-yl]-1-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-ylmethyl)-1-propyl}oxy]methyl dihydrogenphosphate ethanol (1/1/1) 

Relevant academic research and scientific papers

Phosphonooxymethyl prodrugs of the broad spectrum antifungal azole, ravuconazole: Synthesis and biological properties

Synthesis of phosphonooxymethyl derivatives of ravuconazole, 2 (BMS-379224) and 3 (BMS-315801) and their biological evaluation as potential water-soluble prodrugs of ravuconazole are described. The phosphonooxymethyl ether analogue 2 (BMS-379224) and N-ph

PROCESS FOR PRODUCTION OF WATER-SOLUBLE AZOLE PRODRUG

An object of the present invention is to provide a process, or the like, suitable for the industrialization of effective deprotection reaction without using a toxic solvent as well as to provide a process, or the like, for preparing a water-soluble azole prodrug effectively. The present invention provides a process for preparing a salt represented by Formula (I); (wherein X represents a fluorine atom bonded at position 4 or position 5 of a phenyl group) comprising the steps of: (a) carrying out a deprotection reaction of a compound represented by Formula (II); (wherein X represents a fluorine atom bonded at position 4 or position 5 of a phenyl group) in the presence of a carbocation scavenger.

STABILIZED PHARMACEUTICAL COMPOSITION

It is an object of the present invention to provide a pharmaceutical composition containing a stable azole-based compound, which is useful as an antifungal agent. According to the present invention, the above-mentioned object can be achieved by adding magnesium hydroxide carbonate, triethylamine, arginine, or another such basic substance to an azole-based compound that is unstable in acids. The above-mentioned pharmaceutical composition is stable enough that the compound will not degrade if the temperature, humidity, or other such conditions should change during production or storage. Also, this composition is useful as a therapeutic agent for deep mycoses because systemic administration is possible by applying it to an oral agent or an injection.

MONO-LYSINE SALTS OF AZOLE COMPOUNDS

Mono-lysine salts of triazole compounds having a secondary or tertiary hydroxy group are provided. More particularly, the new water-soluble triazole antifungal mono-lysine salt compounds, or solvates thereof, are provided having the general formula I: wherein A in formula I represents the non-hydroxy portion of a triazole antifungal compound of the type containing a secondary or tertiary hydroxyl group. R and R1 in formula I can each be a hydrogen atom or an alkyl group having one to six carbon atoms. The novel water-soluble azole compounds are useful for the treatment of fungal infections and can be administered orally, topically and parenterally.