194798-83-9 Usage
Description
Fosfluconazole is a phosphate prodrug of fluconazole, specifically designed to improve the water solubility and reduce the infusion volume required for intravenous administration. It was launched in Japan for the treatment of candidiasis and cryptococcosis infections. Fluconazole, the active component, is a triazole antifungal agent that selectively inhibits fungal cytochrome P450 sterol C-14 alpha-demethylation, making it effective against serious systemic fungal infections.
Uses
Used in Pharmaceutical Industry:
Fosfluconazole is used as an intravenous injection for the treatment of candidiasis and cryptococcosis infections. It offers a solution to the high-volume infusion issue associated with fluconazole by providing approximately 40-fold higher water solubility, allowing for a substantial reduction in infusion volume. This makes it particularly beneficial for critically ill patients where fluid overload must be avoided.
Used in Antifungal Treatments:
Fosfluconazole is used as an antifungal agent, rapidly hydrolyzed to fluconazole by phosphatase enzymes in vivo. It exhibits similar efficacy to fluconazole in experimental models of fungal disease, providing an effective treatment option for patients with deep-seated mycosis due to Candida or Cryptococcus.
Brand Name:
The brand name for fosfluconazole is Prodif.
Originator
Pfizer (Japan)
Check Digit Verification of cas no
The CAS Registry Mumber 194798-83-9 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,9,4,7,9 and 8 respectively; the second part has 2 digits, 8 and 3 respectively.
Calculate Digit Verification of CAS Registry Number 194798-83:
(8*1)+(7*9)+(6*4)+(5*7)+(4*9)+(3*8)+(2*8)+(1*3)=209
209 % 10 = 9
So 194798-83-9 is a valid CAS Registry Number.
InChI:InChI=1/C13H13F2N6O4P/c14-10-1-2-11(12(15)3-10)13(25-26(22,23)24,4-20-8-16-6-18-20)5-21-9-17-7-19-21/h1-3,6-9H,4-5H2,(H2,22,23,24)
194798-83-9Relevant articles and documents
Preparation method of fosfluconazole
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Paragraph 0063; 0064-0084, (2020/06/17)
The invention provides a preparation method of fosfluconazole. The method comprises the following steps: preparing fluconazole dichlorophosphate: under the protection of nitrogen, controlling the temperature to be-10 DEG C to 0 DEG C, slowly dropwise adding phosphorus oxychloride into a dichloromethane solution of triethylamine, maintaining the temperature to be-10 DEG C to 0 DEG C, performing stirring for 1 hour, slowly dropwise adding a dichloromethane solution of fluconazole, and monitoring the completion of the reaction by TLC; maintaining temperature between-10 DEG C and 0 DEG C, adding water and stirring for 30 minutes, adding inorganic base until the pH value of the water phase is at least 8; and performing standing stratification, separating out the fluconazole, wherein the organicphase contains the fluconazole dichlorophosphate, the fluconazole is prepared through the fluconazole-fluconazole dichlorophosphate-fluconazole dibenzyl phosphate-fosfluconazole ammonium salt-fosfluconazole process, the yield is increased, all intermediates are controllably prepared, the raw materials can be recycled, and raw material waste and organic waste pollution are reduced.
Triazole derivatives useful in therapy
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, (2008/06/13)
The invention provides compounds of formula 1, R1—OP(O)(OH)2??I wherein R1 represents the non-hydroxy portion of a triazole antifungal compound of the type comprising a tertiary hydroxy group; or a pharmaceutically accepta
