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110588-57-3

中文名称 沙康唑
英文名称 SAPERCONAZOLE
CAS 110588-57-3
分子式 C35H38F2N8O4
分子量 672.72
MOL 文件 110588-57-3.mol
110588-57-3 结构式 110588-57-3 结构式

基本信息

中文别名
沙康唑
沙柏康唑
化合物 T16714
4-[4-[4-[4-[[2-(2,4-二氟苯基)-2-(1H-L,2,4-三唑-1-基甲基)- 1,3-二氧戊环-4-基]甲氧基]苯基]-1-哌嗪基]苯基]-2,4-二氢-2-(1-甲基丙基)-3H-1,2,4-三唑-3-酮
英文别名
R-66905
SAPERCONAZOLE
SAPERCONAZOLE USP/EP/BP
a-(2 4-DIFLUOROPHENYL)-a-(1H-1 2 4-TRAIZ OL-1-YLMETHYL)-1H-1 2 4-TRIAZOLE-1-ETHAN OL(FLUCONAZOLE)
2-sec-Butyl-4-[4-[4-[4-[[2-(1H-1,2,4-triazole-1-ylmethyl)-2-(2,4-difluorophenyl)-1,3-dioxolane-4-yl]methoxy]phenyl]-1-piperazinyl]phenyl]-2,4-dihydro-3H-1,2,4-triazole-3-one
4-[4-[4-[4-[[2-(2,4-Difluorophenyl)-2-(1H-1,2,4-triazol-1-yl-methyl)-1,3-dioxolan-4-y1]methoxyl]phenyl]-1-piperazinyl]phenyl]-2,4-dihydrcr2-(1-methylpropyl)-3H-1,2,4-triazol-3-one
3H-1,2,4-Triazol-3-one, 4-[4-[4-[4-[[2-(2,4-difluorophenyl)-2-(1H-1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]-1-piperazinyl]phenyl]-2,4-dihydro-2-(1-methylpropyl)-
SaperconazoleQ: What is Saperconazole Q: What is the CAS Number of Saperconazole Q: What is the storage condition of Saperconazole Q: What are the applications of Saperconazole
2-(1H-1,2,4-Triazol-1-ylmethyl)-2-(2,4-difluorophenyl)-4-[[4-[4-[4-[[2-(1-methylpropyl)-2,3-dihydro-3-oxo-4H-1,2,4-triazol]-4-yl]phenyl]piperazin-1-yl]phenoxy]methyl]-1,3-dioxolane
(+-)-1-sec-Butyl-4-(p-(4-(p-(((2R*,4S*)-2-(2,4-difluorophenyl)-2-(1H-1 ,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl)methoxy)phenyl)-1-piperazin yl)phenyl)-delta(sup 2)-1,2,4-triazolin-5-one
所属类别
药物: 抗病源性微生物药: 抗真菌感染药物

物理化学性质

外观性状从乙腈中结晶,熔点189.5℃。难溶于水。
熔点189.5°
沸点812.5±75.0 °C(Predicted)
密度1.37±0.1 g/cm3(Predicted)
储存条件2-8°C
溶解度Soluble in DMSO
酸度系数(pKa)6.47±0.40(Predicted)
形态Solid
颜色Off-white to light yellow

应用领域

用途1
抗真菌药。

制备方法

方法1
化合物(I)和甘油在甲磺酸催化下,回流缩合。产物经3,5-二硝基苯甲酰氯酰化后,用硅胶柱色谱分离出顺式。水解脱去3,5-二硝基苯甲酰基,甲磺酰氯酰化后得到化合物(Ⅱ)。
化合物(Ⅲ)经烷基化后,再水解,得化合物(Ⅳ)。
化合物(Ⅱ)和(Ⅳ)在碱催化下缩合,得沙康唑。

常见问题列表

生物活性
Saperconazole (R66905) 是一种广谱的抗真菌性三唑,具有很强的抗曲霉菌活性,其 MIC90 值为 0.19 mg/L。
靶点

MIC90: 0.19 mg/L

体外研究

The antifungal activity of Saperconazole is complete at 1 μg/mL for all but one strain of A. niger . Eighty percent of all strains show complete absence of growth at 0.1 μg/mL (85% for A. fumigatus ), and this result persists during 14 days of the test.

体内研究

All control pigeons infect with A. fumigatus die within 2 to 5 days. They have necrotic foci in the lungs, air sacs, liver, spleen, and kidneys. These organs are highly positive by histology and oncultures. Saperconazole administered at 2.5 mg/kg is not active, but when it is given at 5 or 10 mg/kg, 92 or 100%, respectively, survive and organ cultures are negative. No drug-related side effects are observed in the pigeons.

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