2-(2,4-DIFLUOROPHENYL)-1,3-BIS(1H-1,2,4-TRIAZOL-1-YL)PROPYL DIHYDROGEN PHOSPHATE

 化学構造式
1807913-50-3
CAS番号.
1807913-50-3
化学名:
别名:
英語名:
2-(2,4-DIFLUOROPHENYL)-1,3-BIS(1H-1,2,4-TRIAZOL-1-YL)PROPYL DIHYDROGEN PHOSPHATE
英語别名:
FOSFLUCONAZOLE;FosflucozoleImpurity4;Fosfluconazole Impurity 4;FLUCONAZOLE DIHYDROGEN PHOSPHATE;2-(2,4-DIFLUOROPHENYL)-1,3-BIS(1H-1,2,4-TRIAZOL-1-YL)PROPYL DIHYDROGEN PHOSPHATE;2-(2,4-Difluorophenyl)-1,3-di(1h-1,2,4-triazol-1-yl)propan-2-yl hydrogen phosphonate;Phosphonic acid, mono[1-(2,4-difluorophenyl)-2-(1H-1,2,4-triazol-1-yl)-1-(1H-1,2,4-triazol-1-ylmethyl)ethyl] ester
CBNumber:
CB6200893
化学式:
C13H13F2N6O3P
分子量:
370.25
MOL File:
Mol file

2-(2,4-DIFLUOROPHENYL)-1,3-BIS(1H-1,2,4-TRIAZOL-1-YL)PROPYL DIHYDROGEN PHOSPHATE 物理性質

沸点 :
653.0±65.0 °C(Predicted)
酸解離定数(Pka):
1.80±0.10(Predicted)

安全性情報

2-(2,4-DIFLUOROPHENYL)-1,3-BIS(1H-1,2,4-TRIAZOL-1-YL)PROPYL DIHYDROGEN PHOSPHATE 価格

メーカー 製品番号 製品説明 CAS番号 包装 価格 更新時間 購入

2-(2,4-DIFLUOROPHENYL)-1,3-BIS(1H-1,2,4-TRIAZOL-1-YL)PROPYL DIHYDROGEN PHOSPHATE 化学特性,用途語,生産方法

説明

Fosfluconazole, a phosphate prodrug of fluconazole (96), was recently approved for intravenous use in Japan in October 2003. The drug was developed as a water-soluble prodrug by Pfizer as an enhancement to the injectable infusion formulation of fluconazole (96), a very potent antifungal agent, that could be used intravenously in bolus doses requiring smaller volumes of fluid and sodium.

合成

The disclosed manufacturing route of synthesis utilized fluconazole (96) as a precursor and was prepared in two steps using inexpensive starting materials. Fluconazole was dissolved in dichloromethane with pyridine and was treated sequentially with phosphorus trichloride at ¨C13??C and reacted at 13??C for 2 hr followed by an addition of benzyl alcohol at 14-16??C and reacted for 2 hrs at 10-15??C. The mixture was then cooled to 0??C and 30% hydrogen peroxide was added over three hours, maintaining the temperature below 20??C. After stirring the reaction at 20??C for 1hr, the intermediate 97 was isolated in 66% yield. Hydrogenation of the benzyl phosphate at 60 psi in water with 5% palladium on carbon gave the desired phosphate prodrug, fosfluconazole (XI) in 88% yield.

説明図

2-(2,4-DIFLUOROPHENYL)-1,3-BIS(1H-1,2,4-TRIAZOL-1-YL)PROPYL DIHYDROGEN PHOSPHATE 上流と下流の製品情報

原材料

準備製品


2-(2,4-DIFLUOROPHENYL)-1,3-BIS(1H-1,2,4-TRIAZOL-1-YL)PROPYL DIHYDROGEN PHOSPHATE 生産企業

Global( 18)Suppliers
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Standardpharm Co. Ltd.
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Shanghai Sunway Pharmaceutical Technology Co.,Ltd. 021-51816796-820 13611835272
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1807913-50-3()キーワード:


  • 1807913-50-3
  • FOSFLUCONAZOLE
  • FLUCONAZOLE DIHYDROGEN PHOSPHATE
  • Fosfluconazole Impurity 4
  • 2-(2,4-Difluorophenyl)-1,3-di(1h-1,2,4-triazol-1-yl)propan-2-yl hydrogen phosphonate
  • Phosphonic acid, mono[1-(2,4-difluorophenyl)-2-(1H-1,2,4-triazol-1-yl)-1-(1H-1,2,4-triazol-1-ylmethyl)ethyl] ester
  • FosflucozoleImpurity4
  • 2-(2,4-DIFLUOROPHENYL)-1,3-BIS(1H-1,2,4-TRIAZOL-1-YL)PROPYL DIHYDROGEN PHOSPHATE
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